@article{mehta_patel_patel_patel_shah_rathod_shah_patel_bambharoliya_2024, title={Molecular Docking, In silico ADMET Study and Synthesis of Quinoline Derivatives as Dihydrofolate Reductase (DHFR) Inhibitors: A Solvent-free One-pot Green Approach through Sonochemistry}, volume={21}, ISSN={["1875-628X"]}, DOI={10.2174/1570180820666221107090046}, abstractNote={ Quinoline derivatives have evinced their biological importance in targeting bacteria by inhibiting Dihydrofolate reductase. H2SO4 was successfully applied as an acid catalyst for a green, efficient, and one-pot solvent-free synthesis of quinoline derivatives using sonochemistry approach from various aromatic amines and glycerol with affording yield up to 96% within 6-10 min. In this study, the synthesis, characterization, and biological assessment of fifteen quinoline derivatives (1-15) as potential DHFR inhibitors were carried out. The target compounds were docked to study the molecular interactions and binding affinities with the 1DLS enzyme. The synthesized molecules were characterized using IR, MASS, and 1H and 13C NMR. The In-silico molecular docking study was carried out through target Human Dihydrofolate Reductase (DHFR) retrieved from a protein data bank having PDB ID: 1DLS and the antimicrobial activity of all synthesized compounds were tested against Human Dihydrofolate Reductase(DHFR) enzyme by using in-vitro DHFR assay kit. The molecular docking results revealed that compounds 2 and 6 have the lowest binding energy and good binding affinity with the DHFR enzyme. In-silico ADMET predictions revealed that all best-scored compounds had good absorption and drug-like properties for potential use as DHFR inhibitors to treat bacterial infection. The in vitro studies revealed that compounds 2 and 6 show potent DFHR inhibitory activity against gram-positive and gram-negative with IC50 = 12.05 ± 1.55 μM and 10.04 ± 0.73 μM, respectively. While compounds 12, 13, and 15 exhibited moderate antimicrobial activity through DHFR inhibition with IC50= 16.33 ± 0.73 μM, 17.02 ± 1.55 μM, and 18.04 ± 1.05 μM, respectively. This environmentally benign sonochemistry-based approach for synthesizing quinoline derivatives could be affordable for large-scale production and become a potential lead candidate for developing a new quinoline-based antimicrobial agent. }, number={3}, journal={LETTERS IN DRUG DESIGN & DISCOVERY}, author={Mehta, Meshwa and Patel, Stuti and Patel, Ashish and Patel, Yug and Shah, Drashti and Rathod, Keyur and Shah, Umang and Patel, Mehul and Bambharoliya, Tushar}, year={2024}, pages={504–519} } @misc{patel_patel_shah_patel_savaliya_bambharoliya_shah_mahavar_patel_2024, title={Unlocking the Potential: A Comprehensive Review for the Synthesis of Benzofuran Derivatives}, volume={11}, ISSN={["2213-347X"]}, DOI={10.2174/0122133461272081231102061911}, abstractNote={ Benzofuran, a versatile heterocyclic compound, has gained considerable attention in recent years due to its diverse biological activities, distinctive structural characteristics, broad synthetic approaches, and extensive applications. The growing potential inherent in benzofuran encourages many researchers to address the challenges of the synthesis of its framework. This comprehensive review aims to provide a detailed overview of the recent advancements in the synthesis of diverse benzofuran derivatives, highlighting innovative strategies, synthetic methodologies, and significant breakthroughs in the field. The synthetic methodologies are classified as metalcatalyzed routes, green-solvent-based routes, microwave-assisted methods, catalyst-free and solvent- free methods, and a miscellaneous group of routes. This categorization in review provides an easy means for the reader to rationally select the best possible synthetic method for benzofuran derivatives. In addition, it explores the use of different solvents and catalysts in benzofuran synthesis, which serves as a valuable resource for chemists, researchers, and scientists involved in pharmaceutical and allied sciences. Overall, this review provides a comprehensive overview of the synthesis of benzofuran scaffolds and complies with all the significant developments in the synthetic routes of benzofuran, which will be useful for researchers interested in the development of new benzofuran-based molecules. }, number={1}, journal={CURRENT GREEN CHEMISTRY}, author={Patel, Krina and Patel, Heli and Shah, Drashti and Patel, Dharti and Savaliya, Neel and Bambharoliya, Tushar and Shah, Ashish and Mahavar, Anjali and Patel, Ashish}, year={2024}, pages={12–36} } @misc{patel_shah_patel_patel_mehta_bambharoliya_2023, title={A Review on Recent Development of Novel Heterocycles as Acetylcholinesterase Inhibitor for the Treatment of Alzheimer's Disease}, volume={24}, ISSN={["1873-5592"]}, DOI={10.2174/1389450124666221213114500}, abstractNote={Alzheimer's Disease (AD), affecting a large population worldwide, is characterized by the old population's loss of memory and learning ability. Cholinergic deficiency is associated with AD, and various cholinesterase inhibitors have been developed to treat AD, including naturally-derived inhibitors, synthetic analogs, and hybrids. Acetylcholinesterase (AChE) has obtained a renewed interest as a therapeutic target in Alzheimer's disease (AD) due to increased neural cells' function by increasing the concentration of acetylcholine. In this review, we reported the recent development of novel heterocyclic compounds such as coumarin-benzotriazole hybrids, carbazole derivatives, tacrine conjugates, N-benzyl-piperidine-aryl-acyl hydrazones hybrid, spiropyrazoline derivatives, coumarin-dithiocarbamate hybrids, etc. as AChE inhibitors for the treatment of Alzheimer disease. All the bioactive compounds show an effect on different cells and interact simultaneously with the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE with a narrow range of IC50 values from 0.4 nm to 88.21 µm using Ellman's in vitro AChE assay method and show high BBB permeability in-vitro. In addition, the in-vitro fluorescence assay study using Amplex Red assay kits revealed that all the compounds could inhibit self-induced β-amyloid (Aβ) aggregation with the highest inhibition range from 31.4 to 82%. Furthermore, most of the compounds show a low toxicity profile during in vivo studies. The results suggest that all the compounds constitute promising leads for the AChE targeted approach for Alzheimer's disease.}, number={3}, journal={CURRENT DRUG TARGETS}, author={Patel, Ashish and Shah, Drashti and Patel, Yug and Patel, Stuti and Mehta, Meshwa and Bambharoliya, Tushar}, year={2023}, pages={225–246} } @article{patel_bambharoliya_shah_patel_patel_shah_patel_mahavar_patel_2023, title={Emerging green synthetic routes for thiazole and its derivatives: Current perspectives}, ISSN={["1521-4184"]}, DOI={10.1002/ardp.202300420}, abstractNote={This review article provides an overview of the green synthesis of thiazole derivatives, emphasizing sustainable and environmentally friendly methodologies. Thiazole derivatives possess significant value and find diverse applications across various fields. However, conventional synthesis methods often involve hazardous reagents and generate substantial waste, posing environmental concerns. The green synthesis of thiazole derivatives employs renewable starting materials, nontoxic catalysts, and mild reaction conditions to minimize environmental impact. Innovative techniques such as microwave irradiation, ultrasound synthesis, green solvents, a green catalyst-based approach, and mechanochemistry-mediated synthesis are employed, offering advantages in terms of scalability, cost-effectiveness, and purification simplicity. The resulting thiazole derivatives exhibit comparable or enhanced biological activities, showcasing the feasibility and practicality of green synthesis in drug discovery. This review paper underscores the importance of sustainable approaches in functional molecular synthesis and encourages further research in this domain.}, journal={ARCHIV DER PHARMAZIE}, author={Patel, Maitri and Bambharoliya, Tushar and Shah, Drashti and Patel, Krina and Patel, Mehul and Shah, Umang and Patel, Swayamprakash and Mahavar, Anjali and Patel, Ashish}, year={2023}, month={Nov} } @misc{patel_patel_patel_patel_bambharoliya_2023, title={Mini Review on Cariprazine: A Promising Antipsychotic Agent}, volume={22}, ISSN={["1996-3181"]}, url={https://doi.org/10.2174/1871527321666220324121935}, DOI={10.2174/1871527321666220324121935}, abstractNote={Cariprazine is a piperazine derivative approved by the USFDA in 2015 as a novel atypical antipsychotic drug (APD) to treat adults with schizophrenia and bipolar manic or mixed episodes in adults. However, due to the partial agonist action on dopamine D2, D3 receptors, and serotonin 5-HT1A receptors as well as antagonist effect on 5-HT2A, 5-HT2B, and H1 receptors, cariprazine differentiate pharmacologically from other APDs, both typical and atypical. Moreover, cariprazine also has a unique pharmacokinetic profile due to the formation of two clinically significant metabolites: desmethyl-cariprazine (DCAR), longer half-life than parent cariprazine and didesmethyl-cariprazine (DDCAR) by CYP3A4, and also lower extent through CYP2D6. Here, we also review the effectiveness, safety, as well as current clinical update of cariprazine in bipolar I disorder associated with/without mania and schizophrenia by randomized and post-hoc analysis. The potential benefits of cariprazine as a promising therapeutic alternative in addressing major clinical requirements for better therapy of such severe neuropsychiatric conditions were demonstrated in this summarized review study.}, number={2}, journal={CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS}, author={Patel, Ashish and Patel, Arya and Patel, Darshini and Patel, Krina and Bambharoliya, Tushar}, year={2023}, pages={226–236} } @article{patel_bambharoliya_shah_patel_savaliya_patel_patel_bhavsar_patel_patel_et al._2023, title={Recent Progress for the Synthesis of ss-Carboline Derivatives - an Update}, ISSN={["1563-5333"]}, DOI={10.1080/10406638.2023.2180525}, abstractNote={The β-Carboline and its derivatives are privileged heterocyclic motifs and important building blocks in the field of medicinal chemistry due to their remarkable pharmacological potentialities and their derivatives have attracted a great deal of interest due to their wide range of biological activities. β-Carboline contains tricyclic pyrido[3,4-b]indole moiety in their structure. The growing potential inherent in them encourages many researchers to address the challenges of the synthesis of β-Carboline framework. As a result, many methodologies have been developed to synthesize this important class of compounds. The present review is mainly an attempt to present the research work reported in the recent scientific literature focusing on different synthetic methods of β-Carboline and related derivatives.}, journal={POLYCYCLIC AROMATIC COMPOUNDS}, author={Patel, Vidhi and Bambharoliya, Tushar and Shah, Drashti and Patel, Yug and Savaliya, Neel and Patel, Yash and Patel, Riddhisiddhi and Bhavsar, Vashisth and Patel, Harnisha and Patel, Mehul and et al.}, year={2023}, month={Feb} } @misc{shah_bambharoliya_patel_patel_patel_nagani_bhavsar_mahavar_patel_2023, title={Sustainable Synthesis of Phenazines: A Review of Green Approaches}, volume={27}, ISSN={["1875-5348"]}, DOI={10.2174/0113852728257006230921091216}, abstractNote={ Owing to its momentous significance in the development of new medications, phenazine, and its analogues are successful heterocyclic scaffolds as well as essential building blocks for developing physiologically active chemicals. Traditionally, phenazine and its derivatives have been synthesized using chemical methods that involve toxic organic solvents, dangerous reagents, and the risk of hazardous metal contamination in the final products. These drawbacks have significantly limited the widespread application of phenazine derivatives in therapeutic treatments and the pharmaceutical industry. Consequently, there is a growing demand for environmentally friendly methods that can address these challenges with less environmental damage. As a result, it is now possible to employ green and highly efficient methods for the synthesis of phenazine and its derivatives. These methods include mechanosynthesis, solvent-free and catalyst-free synthesis, green solvent-based synthesis, ultrasound-assisted synthesis, microwave-assisted synthesis, and other similar approaches. In light of the fact that the phenazine backbone is a widely present biologically active component and the growing need to decrease the use of hazardous solvents, catalysts, and energy, this review has provided a summary of various sustainable and facile synthetic strategies of phenazine derivatives. }, number={13}, journal={CURRENT ORGANIC CHEMISTRY}, author={Shah, Drashti and Bambharoliya, Tushar and Patel, Dharti and Patel, Krina and Patel, Niyati and Nagani, Afzal and Bhavsar, Vashisth and Mahavar, Anjali and Patel, Ashish}, year={2023}, pages={1143–1163} } @article{shah_patel_patel_mehta_patel_bhimani_bambharoliya_2023, title={Ultrasound-Assisted Synthesis of Benzimidazole Derivatives: A Catalyst-Free Green Chemistry Approach}, volume={59}, ISSN={["1608-3393"]}, DOI={10.1134/S1070428023080146}, number={8}, journal={RUSSIAN JOURNAL OF ORGANIC CHEMISTRY}, author={Shah, Drashti and Patel, Ashish and Patel, Stuti and Mehta, Meshwa and Patel, Yug and Bhimani, Bhargav and Bambharoliya, Tushar}, year={2023}, month={Aug}, pages={1397–1406} } @misc{patel_patel_mehta_patel_patel_shah_patel_shah_patel_patel_et al._2022, title={A review on synthetic investigation for quinoline- recent green approaches}, volume={15}, ISSN={["1751-7192"]}, url={https://publons.com/publon/51628205/}, DOI={10.1080/17518253.2022.2064194}, abstractNote={ABSTRACT Quinolines are a prominent heterocyclic motif and crucial building blocks in creating physiologically active compounds. Due to the fast development of novel medicines with a quinoline nucleus, numerous research papers have been published in a short amount of time. Therefore, to comprehend the present state of the quinoline nucleus in medicinal chemistry science, it is necessary to combine new information with older data. So far, several traditional synthesis techniques have been reported in the literature to synthesize this scaffold. Pfitzinger, Gould–Jacob, Friedlander, Skraup, Doebner–von Miller, and Conrad–Limpach are examples of old synthetic methods. However, they need expensive and demanding conditions, such as high temperature, the use of non-biodegradable chemical compounds degrade the ecosystem, create irritation or harm as pollutants, and represent a threat to the environment. However, traditional synthesis processes need a difficult and time-consuming apparatus set-up, resulting in high costs and pollutants. As a result, scientists are presently developing new and innovative techniques to decrease the use of chemicals, solvents, and catalysts, which are detrimental to both humans and the environment. Therefore, we have attempted to shed light in this current review on various reactions to produce quinolines and their derivatives using various green synthetic methods. GRAPHICAL ABSTRACT}, number={2}, journal={GREEN CHEMISTRY LETTERS AND REVIEWS}, author={Patel, Ashish and Patel, Stuti and Mehta, Meshwa and Patel, Yug and Patel, Rushi and Shah, Drashti and Patel, Darshini and Shah, Umang and Patel, Mehul and Patel, Swayamprakash and et al.}, year={2022}, month={Apr}, pages={336–371} } @misc{patel_vanecha_patel_patel_shah_bambharoliya_2022, title={Development of Natural Bioactive Alkaloids: Anticancer Perspective}, volume={22}, ISSN={["1875-5607"]}, url={https://doi.org/10.2174/1389557521666210712111331}, DOI={10.2174/1389557521666210712111331}, abstractNote={Cancer is a frightful disease that still poses a 'nightmare' worldwide, causing millions of casualties annually due to one of the human race's most significant healthcare challenges that requires a pragmatic treatment strategy. However, plants and plant-derived products revolutionize the field as they are quick, cleaner, eco-friendly, low-cost, effective, and less toxic than conventional treatment methods. Plants are repositories for new chemical entities and have a promising cancer research path, supplying 60% of the anticancer agents currently used. Alkaloids are important chemical compounds that serve as a rich reservoir for drug discovery and development. However, some alkaloids derived from natural herbs display anti-proliferation and antimetastatic activity on different forms of cancer, both in vitro and in vivo. Alkaloids have also been widely formulated as anticancer medications, such as camptothecin and vinblastine. Still, more research and clinical trials are required before final recommendations can be made on specific alkaloids. This review focuses on the naturally-derived bioactive alkaloids with prospective anticancer properties based on the information in the literature.}, number={2}, journal={MINI-REVIEWS IN MEDICINAL CHEMISTRY}, publisher={Bentham Science Publishers Ltd.}, author={Patel, Ashish and Vanecha, Ravi and Patel, Jay and Patel, Divy and Shah, Umang and Bambharoliya, Tushar}, year={2022}, pages={200–212} } @article{patel_gandhi_shah_patel_chhatbar_shah_patel_patel_bambharoliya_2022, title={In silico Study and Solvent-free one-pot Synthesis of Tetrahydropyrimidine derivatives by Mechanochemistry Approach for Targeting Human Neutrophil Elastase against Lung Cancer}, volume={18}, ISSN={["1875-6697"]}, DOI={10.2174/1573409918666220622232501}, abstractNote={BACKGROUND Pyrimidine derivative has evinced its biological importance in targeting lung cancer by inhibiting neutrophil elastase. METHODS All THPM derivatives synthesized by the grindstone method at ambient temperature followed by molecular docking study for efficient binding interaction of THPM compounds by targeting human neutrophil elastase (HNE) (PDB ID: 5A0A) and In-silico ADMET study using PkCSM. Moreover, All synthesized compounds were characterized by spectroscopy techniques and screened for anti-cancer activity using in vitro HNE assay kit. RESULTS We reported a one-pot solvent-free mechanochemical approach for synthesizing tetrahydropyrimidine (THPM) derivatives from various aromatic aldehydes, ethyl cyanoacetate, and urea, followed by in silico study and evaluation against human neutrophil elastase (HNE) for treatment of lung cancer. We calibrated the best molecules that bind to specific targets more efficiently using a molecular docking approach and provided the desired efficacy. In-silico ADMET studies revealed that all best-scored compounds had drug-like characteristics for potential use as human neutrophil elastase inhibitors (HNE) in lung cancer treatment. Additionally, the in vitro studies revealed that compounds 1, 2, and 8 show potent HNE inhibitory activity for lung cancer treatment. CONCLUSION In a nutshell, the tetrahydropyrimidine (THPM) scaffold and its derivatives may serve as potential HNE inhibitors for the development of a promising anti-cancer agent.}, number={4}, journal={CURRENT COMPUTER-AIDED DRUG DESIGN}, author={Patel, Ashish and Gandhi, Karan and Shah, Sweta and Patel, Darshan and Chhatbar, Shreyas and Shah, Drashti and Patel, Stuti and Patel, Harnisha and Bambharoliya, Tushar}, year={2022}, pages={293–306} } @misc{patel_patel_mehta_patel_langaliya_bhalodiya_bambharoliya_2022, title={Recent Update on the Development of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors: A Promising Target for the Treatment of Parkinson's Disease}, volume={18}, ISSN={["1875-6638"]}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85131678836&partnerID=MN8TOARS}, DOI={10.2174/1573406418666220215122136}, abstractNote={Parkinson's disease is a relatively common neurological disorder with incidence increasing with age. Since current medications only relieve the symptoms and do not change the course of the disease, therefore, finding disease-modifying therapies is a critical unmet medical need. However, significant progress in understanding how genetics underpins Parkinson's disease (PD) has opened up new opportunities for understanding disease pathogenesis and identifying possible therapeutic targets. One such target is leucine-rich repeat kinase 2 (LRRK2), an elusive enzyme implicated in both familial and idiopathic PD risk. As a result, both academia and industry have promoted the development of potent and selective inhibitors of LRRK2. In this review, we have summarized recent progress on the discovery and development of LRKK2 inhibitors as well as the bioactivity of several small-molecule LRRK2 inhibitors that have been used to inhibit LRRK2 kinase activity in vitro or in vivo.}, number={7}, journal={MEDICINAL CHEMISTRY}, author={Patel, Ashish and Patel, Stuti and Mehta, Meshwa and Patel, Yug and Langaliya, Dhruv and Bhalodiya, Shyam and Bambharoliya, Tushar}, year={2022}, pages={757–771} } @misc{patel_shah_shah_bambharoliya_patel_panchal_parikh_nagani_patel_vaghasiya_et al._2021, title={A Review on the Synthetic Approach of Marinopyrroles: A Natural Anti-tumor Agent from the Ocean}, volume={18}, ISSN={["1875-6255"]}, url={https://publons.com/publon/33252564/}, DOI={10.2174/1570178617999200718004012}, abstractNote={ Natural products play an important role in various drug discovery and development approaches. They are known to be the rich resources for the identification of new chemical entities (NCEs) intended to treat various diseases. Many drugs have been discovered and developed from natural sources. Indeed, collaborative efforts involving biologists as well as organic, medicinal, and phytochemists usually facilitate the identification of potent NCEs derived from natural sources. Over the past 20 years, more than 50% of NCEs have been derived either from marine sources or synthetic/ semisynthetic derivatives of natural products. Indeed, many drug molecules have been designed by considering natural products as the starting scaffold. The first bis-pyrrole alkaloid derivative of marinopyrroles was obtained from the marine-derived streptomycete species. In the laboratory, it can be synthesized via Clauson-Kaas and Friedel-Crafts arylation as well as copper-mediated N-arylation process under microwave irradiation. The marinopyrrole A (±)-28 was discovered to overcome resistance against human cancer cells by antagonizing B-cell lymphoma extra-large (Bcl-xL) and induced myeloid leukaemia cell (Mcl-1). In this review, we elaborated on various synthetic pathways of marinopyrroles possessing anti-cancer potential, which could encourage researchers to discover promising anti-tumor agents. }, number={4}, journal={LETTERS IN ORGANIC CHEMISTRY}, author={Patel, Ashish and Shah, Hirak and Shah, Umang and Bambharoliya, Tushar and Patel, Mehul and Panchal, Ishan and Parikh, Vruti and Nagani, Afzal and Patel, Harnisha and Vaghasiya, Jitendra and et al.}, year={2021}, pages={251–264} } @article{zhang_bambharoliya_xie_liu_celik_wang_akkus_king_2021, title={A hybrid vascular graft harnessing the superior mechanical properties of synthetic fibers and the biological performance of collagen filaments}, volume={118}, ISSN={["1873-0191"]}, url={https://publons.com/publon/37769973/}, DOI={10.1016/j.msec.2020.111418}, abstractNote={Tissue-engineered small caliber vascular grafts have attracted much research attention as a viable alternative to traditional vascular grafts with their biocompatibility and potential to achieve complete healing. However, the major challenge is to fabricate a scaffold with both satisfactory mechanical properties and fast endothelialization. In this study, a hybrid tubular vascular tissue engineered scaffold has been circular-knitted using novel electrochemically aligned collagen (ELAC) filaments plied together with traditional poly(lactic acid) (PLA) yarn. The collagen component was able to promote the recruitment and proliferation of endothelial cells by increasing the initial cell adhesion 10-fold and the eventual cell population 3.2 times higher than the PLA scaffold alone. At the same time, the PLA yarn was able to provide sufficient mechanical strength and structural stability, as well as facilitate scaffold fabrication on high speed textile production equipment. The tubular hybrid scaffold exhibited excellent bursting strength (1.89 ± 0.43 MPa) and suture retention strength (10.86 ± 0.49 N), and had comparable compliance (3.98 ± 1.94%/100 mmHg) to that of the coronary artery (3.8 ± 0.3%/100 mmHg) under normotensive pressure. With its excellent mechanical and biological performance, this prototype hybrid scaffold is a promising candidate for the construction of a clinically successful and easily translatable tissue-engineered small caliber vascular graft.}, journal={MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS}, publisher={Elsevier BV}, author={Zhang, Fan and Bambharoliya, Tushar and Xie, Yu and Liu, Laijun and Celik, Hakan and Wang, Lu and Akkus, Ozan and King, Martin W.}, year={2021}, month={Jan} } @article{patel_shah_patel_patel_soni_nagani_parikh_shah_bambharoliya_2021, title={Benzimidazole as Ubiquitous Structural Fragment: An Update on Development of its Green Synthetic Approaches}, volume={18}, ISSN={["1875-6298"]}, url={https://doi.org/10.2174/1570193X17999201211194908}, DOI={10.2174/1570193X17999201211194908}, abstractNote={ The benzimidazole and its derivatives are privileged heterocyclic motif and important building block for the development of the biologically active compound. However, several research reports are produced in a short period of time due to the rapid production of new drugs having a benzimidazole nucleus. In order to understand the current status of the benzimidazole nucleus in medicinal chemistry science, it is therefore important to combine the latest knowledge with earlier information. Hence, synthetic organic chemists concentrated on inventing an effective green methodology for synthesizing benzimidazole derivatives. In addition to this, non-degradable chemical compounds cause the ecosystem to become fragile, damage or irritation as contaminants and pose a danger to the environment. However, conventional methods of synthesis need longer heating time, complicated and tedious apparatus set up which result in high cost and pollution in contrast to greener methods which are inexpensive. In the present review, therefore, we have attempted to shed light on various synthetic strategies leading to the synthesis of different benzimidazole derivatives through the direct condensation reaction between o-phenylenediamine and aromatic aldehydes using green chemistry approaches such as mechanochemistry, ultrasound irradiation, microwave irradiation, environmentally benign solvents/catalysts, reactant immobilized on a solid support and blue light irradiation. }, number={8}, journal={MINI-REVIEWS IN ORGANIC CHEMISTRY}, publisher={Bentham Science Publishers Ltd.}, author={Patel, Ashish and Shah, Drashti and Patel, Naiya and Patel, Khushbu and Soni, Nidhi and Nagani, Afzal and Parikh, Vruti and Shah, Hirak and Bambharoliya, Tushar}, year={2021} } @article{patel_patel_hemani_solanki_kansara_patel_pradhan_bambharoliya_2021, title={Exploring the in-silico approach for assessing the potential of natural compounds as a SARS-CoV-2 main protease inhibitors}, volume={14}, ISSN={["1307-6175"]}, url={https://publons.com/publon/45416080/}, DOI={10.25135/ACG.OC.97.2012.1895}, abstractNote={The SARS-CoV-2 virus emerged as a major cause of the COVID-19 pandemic in December 2019 Many attempts have been made to block the viral infection by targeting various processes like its entry, uncoating, replication, activating T cells response, and rising antibody titer Also, many drugs are repurposed like remdesivir, dexamethasone, tocilizumab, hydroxychloroquine based on their established therapeutic efficacy against other viruses in the past Natural products (NP) consist of a promising candidate and are needed to evaluate those molecules with molecular docking for preliminary screening and in vitro studies Therefore, in the present study, a total of 12 active constituents from natural products like Ashwagandha, Tinospora cordifolia, Tea, Neem and lemon balm were docked, using the Autodock tool, onto the crystal structure of SARS CoV-2 main protease (PDB ID-5R80), to study their capability to act as main protease (Mpro) COVID-19 inhibitors All NPs derivatives displayed good binding energies (Delta G) ranging from -8 8 to -5 2 kcal/mol, but berberine, epicatechin, and rosmarinic acid were found most potent, among others Therefore, good binding energy, drug-likeness, and efficient pharmacokinetics suggest the potential of NPs derivatives as SARS-CoV-2 main protease (Mpro) inhibitors However, further research is necessary to investigate the ability of these compounds as COVID-19 inhibitors (C) 2021 ACG Publication All right reserved}, number={1}, journal={ORGANIC COMMUNICATIONS}, author={Patel, Ashish and Patel, Alkesh and Hemani, Rahul and Solanki, Riddhi and Kansara, Janki and Patel, Gargi and Pradhan, Sayantan and Bambharoliya, Tushar}, year={2021}, pages={58–72} } @misc{patel_shah_patel_patel_soni_nagai_shah_patel_patel_bhimani_et al._2021, title={Quinoxaline as Ubiquitous Structural Fragment: An Update on the Recent Develop-ment of its Green Synthetic Approaches}, volume={25}, ISSN={["1875-5348"]}, url={https://publons.com/publon/51640511/}, DOI={10.2174/1385272825666211125102145}, abstractNote={ Quinoxaline is a versatile heterocyclic moiety that possesses a wide range of biological activities. Therefore, many researchers have been performing the synthesis of quinoxaline derivatives on a daily basis. In addition, high demands for their synthesis often result in an increased generation of different waste chemicals. However, to minimize the utilization and generation of toxic organic substances, the present review focuses on the various green synthetic approaches for the synthesis of quinoxaline and its derivatives. Moreover, due to the quick manufacturing of novel medications using a quinoxaline scaffold, multiple study reports are published in a short period of time. Therefore, to fully comprehend the current state of the quinoxaline scaffold in medicinal chemistry, it is necessary to combine recent findings with previous understanding. Besides, compared to conventional methods, these green methods minimize the use and generation of harmful chemicals and improve reaction efficiency in terms of product yields, purity, energy consumption, and post-synthetic procedures. Therefore, in this review, we have attempted to shed light on various green synthetic strategies leading to the synthesis of quinoxaline scaffold and its derivatives, such as ultrasound irradiation, microwave irradiation, grindstone technique, environmentally benign solvents/catalysts based, and reactant immobilized on a solid support, etc. }, number={24}, journal={CURRENT ORGANIC CHEMISTRY}, author={Patel, Ashish and Shah, Drashti and Patel, Naiya and Patel, Khushbu and Soni, Nidhi and Nagai, Afzal and Shah, Umang and Patel, Mehul and Patel, Swayamprakash and Bhimani, Bhargav and et al.}, year={2021}, pages={3004–3016} } @article{patel_shah_patel_patel_patel_dobaria_shah_patel_chokshi_patel_et al._2021, title={Ultrasound-Assisted One-Pot Synthesis of Tetrahydropyrimidne Derivatives through Biginelli Condensation: A Catalyst Free Green Chemistry Approach}, volume={18}, ISSN={["1875-6255"]}, url={https://publons.com/publon/51640510/}, DOI={10.2174/1570178617999201105162851}, abstractNote={ The aim of present work is one-pot catalyst free green synthesis of tetrahydropyrimidne derivatives through Biginelli condensation under ultrasonic irradiation. The chemical applications of ultrasound, "sonochemistry", has become an exciting new field of research during the past decade as it can increase reactivities by nearly a million fold. Owing to the increasing use of Green technology approach, due to its various merits over Classical methodology and as a need for sustainable Chemistry, this reaction has received renewed interest for preparing tetrahydropyrimidine (THPM) through Biginelii condensation in an environmentally thoughtful manner with improved yields. The objective of the present study is focused on developing novel Ultrasound-Assisted catalyst free one-pot synthesis of tetrahydropyrimidne derivatives through Biginelli condensation We, herein describe a highly efficient catalyst free one-pot green synthesis of tetrahydropyrimidine derivatives using Biginelli protocol under ultrasonic irradiation at 50°C. All the products were characterized by comparing their physical and spectral data with those of authentic compounds reported in the literature. A green and efficient ultrasound-assisted one-pot synthesis method for tetrahydro-yrimidine derivatives have been developed through Biginelli condensation. The technique affords up to 99% yield in only 5–20 minutes under mild heating. Each synthesized compounds were fully characterized through spectral techniques viz. IR, 1H NMR, and Mass Spectroscopy. A green and efficient ultrasound-assisted one-pot synthesis method for tetrahy-droyrimidine derivatives have been developed through Biginelli condensation. The present sonochemistry based green chemistry approach with no additional acid catalyst produces no waste, shows a significant enhancement in reaction rates under mild ultrasound irradiation in excellent yields and therefore represents a green and enviro-economic synthetic methodology for the Biginelli condensation in comparison to conventional heating/micro-wave irradiation. }, number={9}, journal={LETTERS IN ORGANIC CHEMISTRY}, author={Patel, Ashish and Shah, Jinagna and Patel, Kesha and Patel, Krishna and Patel, Harit and Dobaria, Divyesh and Shah, Umang and Patel, Mehul and Chokshi, Avani and Patel, Samir and et al.}, year={2021}, pages={749–756} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Coronary Artery Disease and The Evolution of Angioplasty Devices}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85127797918&partnerID=MN8TOARS}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={1–62} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Coronary Microvascular Dysfunction (CMD)}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85127816902&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_3}, abstractNote={Over the past two decades, coronary microvascular dysfunction (CMD) has emerged as an important mechanism of myocardial ischemia. This chapter describes various pathogenic mechanisms of CMD and explains how CMD can result from functional and/or structural alterations to the vessel wall and lead to varying degrees of disruption to normal coronary physiology. Currently ≈20–50% of patients have a predisposition towards ongoing angina despite successful revascularization surgery. The current goal of percutaneous coronary intervention (PCI) or any other revascularization therapy is to relieve the symptoms rather than address the pathology. It will require new research in this area if an improvement in CMD pathology is to be achieved.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={11–14} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Definitions and Basic Mechanism of Coronary Artery Disease (CAD)}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85127822516&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_2}, abstractNote={Coronary artery disease (CAD) also known as coronary heart disease (CHD) is described as the pathologic process affecting the coronary arteries, while atherosclerotic cardiovascular disease (ASCVD or CVD for short) is referred to as the pathological process affecting the entire arterial circulation, not just the coronary arteries. This chapter defines CAD and CHD along with their atherosclerotic pathogenic pathway and all the factors associated with it. The progression of atherosclerosis and its clinical findings are explained at various stages together with a description of the time course of inflammation and atherosclerotic calcification.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={3–10} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Diagnosis of Coronary Artery Disease (CAD)}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85127790223&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_4}, abstractNote={The evaluation of a patient with known or suspected cardiovascular disease begins with their medical history and a targeted physical examination as well as basic ancillary studies that are sufficient for the physician to understand the aetiology of any chest pain. A history and symptoms of angina are important in order to determine which tools should be used for diagnosis and treatment. This chapter describes the major signs and symptoms associated with cardiac disease. The probability of coronary artery disease (CAD) by age, gender and symptoms are described along with the different types of angina. Invasive and noninvasive techniques that successfully diagnose cardiac disease are also discussed briefly in this chapter. It also includes a comprehensive approach to the diagnosis and treatment of patients with chest pain according to various clinical guidelines. It also lists the established and novel biomarkers for the diagnosis of chronic coronary arterial disease.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={15–20} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Epidemiology and Risk Factors}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85097422057&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_1}, abstractNote={Coronary artery disease (CAD) is a major cause of death and disability in developed countries. Heart disease and stroke are among the top five leading causes of death. This chapter shows the data that CAD is and will continue to become a global burden of disease and, by 2035, nearly half of the US population will have some form of cardiovascular disease (CVD). The American Heart Association has defined seven key risk factors for heart disease and stroke called “Life’s Simple 7”. These are listed in this chapter along with their global impact.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={1–2} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Evolution of Angioplasty Devices}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85118177686&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_6}, abstractNote={It is estimated that 600,000 to 1 million cardiac catheterizations (CC) are performed annually in the United States. This figure exceeds the number of coronary artery bypass graft procedures (CABG) performed on an annual basis, and is expected to grow annually by about 1–5% in the United States. This chapter discusses the evolution in design and development of angioplasty devices including a list of currently available commercial products and experimental designs under research and development. This will enable the reader to get a glimpse of how the medical device sector is attempting to address this major healthcare problem whose total medical costs are expected to reach $1.1 trillion by 2035.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={31–52} } @article{shah_patel_parikh_nagani_bhimani_shah_bambharoliya_2020, title={The β-Secretase Enzyme BACE1: A Biochemical Enigma for Alzheimer’s Disease}, volume={19}, url={https://doi.org/10.2174/1871527319666200526144141}, DOI={10.2174/1871527319666200526144141}, abstractNote={Beta site amyloid precursor protein cleaving enzyme 1 (BACE1) is a rational target in Alzheimer's disease (AD) drug development due to its role in amyloidogenic cleavage of Amyloid precursor protein (APP) in generating Amyloid β (Aβ). This β-secretase cleaves not only Amyloid precursor protein (APP) and its homologues but also small series of substrate including neuregulin and β subunit of voltage gated sodium channel that play a very important role in the development and normal function of the brain. Moreover, BACE1 is modulated at the post translational level by several factors that are associated with both physiological and pathological functions. Since the discovery of BACE1 over a decade ago, medicinal chemistry and pharmacokinetics of BACE1 small molecule inhibitors have proven challenging for the treatment of Alzheimer's disease.}, number={3}, journal={CNS & Neurological Disorders - Drug Targets}, publisher={Bentham Science Publishers Ltd.}, author={Shah, Hirak and Patel, Ashish and Parikh, Vruti and Nagani, Afzal and Bhimani, Bhargav and Shah, Umang and Bambharoliya, Tushar}, year={2020}, month={Aug}, pages={184–194} } @inbook{king_bambharoliya_ramakrishna_zhang_2020, title={Treatment of Coronary Artery Disease (CAD)}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85127733730&partnerID=MN8TOARS}, DOI={10.1007/978-3-030-42443-5_5}, abstractNote={The treatment of a particular patient’s coronary artery disease (CAD) will depend on the severity of the symptoms and the patient’s pathological condition. In addition to pain, patients may suffer from other symptoms, such as severe fatigue, dyspnea, abdominal pain, nausea and sweating. And in order to understand cardiac pain, one requires knowledge of the interplay between ischemic, metabolic and neurological mechanisms behind CAD. This chapter presents the alternative therapies for stable ischemic heart disease (SIHD) and for acute coronary syndrome (ACS), such as drug therapy, invasive therapy and minimally invasive therapy. Reference is made to the National Institute for Health and Care Excellence (NICE) 2011 respective guidelines, which recommend medical therapy for chronic stable angina and reperfusion therapy for patients with STEMI.}, booktitle={SpringerBriefs in Materials}, author={King, M.W. and Bambharoliya, T. and Ramakrishna, H. and Zhang, F.}, year={2020}, pages={21–29} } @inproceedings{bambharoliya_hu_cheng_king_2019, title={Design and development of stent coated with novel cardiac stem cell-mimicking regenerative factors}, volume={40}, url={http://www.scopus.com/inward/record.url?eid=2-s2.0-85065394023&partnerID=MN8TOARS}, booktitle={Transactions of the Annual Meeting of the Society for Biomaterials and the Annual International Biomaterials Symposium}, author={Bambharoliya, T. and Hu, S. and Cheng, K. and King, M.W.}, year={2019}, pages={481} }