Thirumurugan Rathinasabapathy
Also known as: Thiru
Lead Optimization; Preclinical Candidate; Biomarker; Food Chemistry; Natural Product Chemistry
Works (36)
Updated: August 29th, 2023 11:24
2023 journal article
Gel formulated with Bryophyllum pinnatum leaf extract promotes skin wound healing in vivo by increasing VEGF expression: A novel potential active ingredient for pharmaceuticals
FRONTIERS IN PHARMACOLOGY, 13.
author keywords: Crassulaceae; topical gel formulation; wound healing; stability study; analytical marker; phenolic compounds
TL;DR:
The gel formulation containing extract exhibited relevant skin wound healing properties and has the potential to be applied as a novel active ingredient for developing wound healing pharmaceuticals.
(via Semantic Scholar)
www.frontiersin.org (publisher PDF)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: Web Of Science, ORCID
Added: March 20, 2023
2022 review
All Polyphenols Are Not Created Equal: Exploring the Diversity of Phenolic Metabolites
[Review of ]. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 70(7), 2077–2091.
Contributors: C. Vong n, n , M. Moncada n & S. Komarnytsky n
author keywords: (poly)phenols; phenolic acids; microbiome; microbial catabolism; methylation
MeSH headings : Antioxidants; Flavonoids / metabolism; Humans; Phenols / chemistry; Polyphenols / metabolism; Tannins
TL;DR:
There is a critical need for precise identification of the individual phenolic metabolite signatures originating from different polyphenol groups to enable future translation of these findings into break-through nutritional interventions and dietary guidelines.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger
(OpenAlex)
3. Good Health and Well-being
(Web of Science)
Sources: Web Of Science, ORCID
Added: February 12, 2022
2022 review
Plant-Based Support of Respiratory Health during Viral Outbreaks
[Review of ]. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 70(7), 2064–2076.
Contributors: n , L. Sakthivel* & S. Komarnytsky n
author keywords: licorice; coneflower; ginger; mullein; horehound; elderberry; nettle; antiviral; anti-inflammatory; expectorant; COVID-19
MeSH headings : Disease Outbreaks; Humans; Phytotherapy; Plant Extracts / pharmacology; Respiratory System; Virus Diseases / drug therapy
TL;DR:
Investigating metabolites and their botanical sources holds potential to uncover new mediators of the respiratory health outcomes as well as molecular targets for future break-through therapeutic interventions targeting respiratory viral outbreaks.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Sources: Web Of Science, ORCID
Added: February 12, 2022
2021 review
Endocannabinoid System and Its Regulation by Polyunsaturated Fatty Acids and Full Spectrum Hemp Oils
[Review of ]. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 22(11).
Contributors: S. Komarnytsky n , n , C. Wagner n , B. Metzger*, C. Carlisle*, C. Panda *, S. Le Brun-Blashka*, J. Troup*, S. Varadharaj*
author keywords: ECS tone; phytocannabinoids; inflammation resolution; oxidative stress; systemic redox balance
MeSH headings : Adenosine / metabolism; Animals; Cannabinoids / metabolism; Cannabis / metabolism; Diet; Endocannabinoids / metabolism; Fatty Acids, Unsaturated / metabolism; Homeostasis / physiology; Humans; Inflammation / metabolism; Lipid Metabolism / physiology; Oxidative Stress / physiology; Plant Extracts / metabolism; Signal Transduction / physiology; TRPV Cation Channels / metabolism
TL;DR:
Clinical evidence reviewed in this study links PUFAs and cannabinoids to changes in ECS tone, immune function, metabolic and oxidative stress adaptation, and overall maintenance of a well-balanced systemic function of the body.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger
(OpenAlex)
3. Good Health and Well-being
(Web of Science)
Sources: Web Of Science, ORCID
Added: May 24, 2021
2021 journal article
Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 22(3).
Contributors: M. Wilson n, V. Konda*, K. Heidt n, n , A. Desai* & S. Komarnytsky n
author keywords: postmenopausal; estrogens; hot flashes; HRT; ERr 731
MeSH headings : Animals; Biomarkers; Disease Models, Animal; Dose-Response Relationship, Drug; Estrogen Receptor alpha / metabolism; Estrogen Receptor beta / metabolism; Hot Flashes; Menopause / drug effects; Molecular Structure; Ovariectomy; Phytoestrogens / chemistry; Phytoestrogens / pharmacology; Plant Extracts / chemistry; Plant Extracts / pharmacology; Plant Roots / chemistry; Postmenopause; Rats; Rheum / chemistry; Vasomotor System / drug effects
TL;DR:
Data validate the OVX/Tskin rat model as a suitable screening platform to evaluate botanical and pharmaceutical treatments of menopause, while providing further evidence for the efficacy of ERr 731 towards alleviating vasomotor menopausal symptoms and improving wellbeing during the menopausal transition.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
5. Gender Equality
(Web of Science)
Sources: Web Of Science, ORCID
Added: January 21, 2021
2020 journal article
Enhanced stability of berry pomace polyphenols delivered in protein-polyphenol aggregate particles to an in vitro gastrointestinal digestion model
Food Chemistry, 331, 127279.
Contributors: J. Xiong n , Y. Chan n, n , M. Grace n , S. Komarnytsky n & M. Lila n
author keywords: Food matrix; By-product; Stability; Antioxidant; Anti-inflammatory
MeSH headings : Animals; Anthocyanins / analysis; Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics; Antioxidants / analysis; Blueberry Plants / chemistry; Digestion; Food-Processing Industry; Fruit / chemistry; Mice; Plant Extracts / chemistry; Plant Extracts / pharmacokinetics; Plant Proteins, Dietary / chemistry; Polyphenols / pharmacokinetics; Proanthocyanidins / analysis; RAW 264.7 Cells; Vitis / chemistry
TL;DR:
Protein-polyphenol particle digests retained 1.5 to 2-fold higher antioxidant capacity and suppressed the expression of pro-inflammatory cytokines, iNOS, IL6, and IL1β, compared to unmodified extract digests, which only suppressed IL6.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: ORCID
Added: June 19, 2020
2020 journal article
Spicing up gastrointestinal health with dietary essential oils
Phytochemistry Reviews, 19(2), 243–263.
Contributors: M. Tanveer n, C. Wagner n, M. Haq *, N. Ribeiro n, n , M. Butt *, A. Shehzad *, S. Komarnytsky n
author keywords: Essential oils; Indigestion; Gastroesophageal reflux; Dyspepsia; Gastritis
TL;DR:
8 botanical interventions including fennel, rosemary, ginger, peppermint, and dill were identified that prevented gastric ulcer formation, reduced production of gastric acids, or promoted upper gastrointestinal healing in preclinical or early phase human studies.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger
(OpenAlex)
3. Good Health and Well-being
(Web of Science)
Source: ORCID
Added: March 5, 2020
2019 journal article
Distinct fractions of an Artemisia scoparia extract contain compounds with novel adipogenic bioactivity
Frontiers in Nutrition, 6.
Contributors: A. Boudreau*, A. Poulev*, D. Ribnicky*, I. Raskin *, * , A. Richard *, J. Stephens *
author keywords: adipocyte; plants-medicinal; botanical extract; adipogenesis; fat cell; activity-guided fractionation; 3T3-L1 adipocyte
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: July 16, 2022
2018 journal article
Edible foxtail millet flour stabilises and retain the invitro activity of blueberry bioactive components
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY, 53(7), 1771–1780.
Contributors: K. Mak *, * , S. Sankaran*, M. Kandasamy*, E. Ling*, M. Balijepalli*, S. Sagineedu*, M. Pichika *
author keywords: -glucosidase enzyme; anthocyanins; antioxidant; blueberries; foxtail millet flour; polyphenols
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: Web Of Science, ORCID
Added: August 6, 2018
2017 journal article
Structural constraints and importance of caffeic acid moiety for anti-hyperglycemic effects of caffeoylquinic acids from chicory
MOLECULAR NUTRITION & FOOD RESEARCH, 61(9).
Contributors: K. Jackson n, n , D. Esposito n & S. Komarnytsky n
author keywords: Blood glucose; Cell bioenergetics; Diabetes; Dietary supplementation; Metabolic syndrome
MeSH headings : Animals; Cell Line, Tumor; Chicory / chemistry; Gluconeogenesis / drug effects; Hypoglycemic Agents / pharmacology; MAP Kinase Signaling System; Pharmacogenetics; Phosphatidylinositol 3-Kinases / physiology; Plant Roots / chemistry; Quinic Acid / analogs & derivatives; Quinic Acid / pharmacology; Rats; Structure-Activity Relationship
TL;DR:
It is concluded that the caffeic acid moiety was important for suppression of hepatic gluconeogenesis and hyperglycemia, ultimately strengthening the link between dietary interventions based on caffeic Acid-containing plant foods and healthy glucose metabolism.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science
Added: August 6, 2018
2017 journal article
Thiazolopyridines Improve Adipocyte Function by Inhibiting 11 Beta-HSD1 Oxoreductase Activity
Journal of Chemistry, 2017, 1–10.
Contributors: * , K. Palatini Jackson, Y. Thor n, A. Buru *, D. Esposito n , X. Li n , M. Pichika *, A. Hamzah*, S. Komarnytsky n
TL;DR:
The tetrahydrothiazolopyridine moiety served as an active pharmacophore for inhibiting 11β-HSD1 and offered a novel therapeutic strategy to ameliorate metabolic alterations found in obesity and diabetes.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Sources: ORCID, Web Of Science, Crossref
Added: August 6, 2018
2015 book
Effective waste water treatment and its management
In Toxicity and Waste Management Using Bioremediation (pp. 312–334).
Contributors: S. Prabu *, T. Suriyaprakash, R. Kandasamy * & *
UN Sustainable Development Goal Categories
6. Clean Water and Sanitation
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2014 journal article
Process validation: A review
Pharma Times, 46(4), 12–15. http://www.scopus.com/inward/record.url?eid=2-s2.0-84943603029&partnerID=MN8TOARS
Contributors: S. Prabu, T. Suriyaprakash, R. Thirumurugan & A. Shanmugarathinam
Source: ORCID
Added: July 16, 2022
2013 journal article
Acceleration of cutaneous wound healing by brassinosteroids
WOUND REPAIR AND REGENERATION, 21(5), 688–696.
Contributors: D. Esposito *, * , B. Schmidt *, M. Shakarjian*, S. Komarnytsky n & I. Raskin *
MeSH headings : Administration, Topical; Animals; Blotting, Western; Brassinosteroids / pharmacology; Cell Proliferation; Cells, Cultured; Intercellular Adhesion Molecule-1 / drug effects; Intercellular Adhesion Molecule-1 / metabolism; Male; Mice; Mice, Inbred C57BL; Signal Transduction / drug effects; Skin / injuries; Skin / pathology; Transforming Growth Factor beta / drug effects; Transforming Growth Factor beta / metabolism; Tumor Necrosis Factor-alpha / drug effects; Tumor Necrosis Factor-alpha / metabolism; Wound Healing / drug effects
TL;DR:
Topical application of brassinosteroids accelerates wound healing by positively modulating inflammatory and reepithelialization phases of the wound repair process, in part by enhancing Akt signaling in the skin at the edges of the wounds and enhancing migration of fibroblasts in the wounded area.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science
Added: August 6, 2018
2013 journal article
Antiplasmodial activity of cucurbitacin glycosides from Datisca glomerata (C. Presl) Baill
PHYTOCHEMISTRY, 87, 78–85.
author keywords: Datisca glomerata; Cucurbitales; Datiscaceae; Durango root; Bioassay guided fractionation; Cucurbitacin; Antimalarial; Antileishmanial; Cytotoxicity
MeSH headings : Animals; Antimalarials / chemistry; Antimalarials / pharmacology; CHO Cells; Cell Line; Cricetinae; Glycosides / chemistry; Glycosides / pharmacology; Magnoliopsida / chemistry; Molecular Structure; Plants, Medicinal / chemistry; Plasmodium falciparum / drug effects; Rats; Triterpenes / chemistry; Triterpenes / pharmacology
TL;DR:
The traditionally used antimalarial plant, Datisca glomerata (C. Presl) Baill, was subjected to antiplasmodial assay guided fractionation, which led to the isolation of seven cucurbitacin glycosides, datiscosides I-O, along with two known compounds from the aerial parts of D. glomersata, which displayed cytotoxicity against L6 but not CHO mammalian cells.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science
Added: August 6, 2018
2013 journal article
Effects of Pregnane Glycosides on Food Intake Depend on Stimulation of the Melanocortin Pathway and BDNF in an Animal Model
Journal of Agricultural and Food Chemistry, 61(8), 1841–1849.
Contributors: S. Komarnytsky n , D. Esposito n , * , A. Poulev* & I. Raskin *
author keywords: appetite; satiety; body weight; milkweed; Asclepias
MeSH headings : Animals; Appetite / drug effects; Asclepias / chemistry; Brain-Derived Neurotrophic Factor / genetics; Brain-Derived Neurotrophic Factor / metabolism; Cell Line, Tumor; Eating / drug effects; Female; Glycosides / administration & dosage; Humans; Male; Melanocortins / metabolism; Models, Animal; Plant Extracts / administration & dosage; Pregnanes / administration & dosage; Rats; Rats, Wistar
TL;DR:
The results support the multimodal effects of pregnane glycosides on feeding regulation, which depends on the activity of the melanocortin signaling pathway and BDNF.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger
(Web of Science)
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science, Crossref
Added: August 6, 2018
2012 journal article
Antiparasitic compounds from Cornus florida L. with activities against Plasmodium falciparum and Leishmania tarentolae
JOURNAL OF ETHNOPHARMACOLOGY, 142(2), 456–461.
Contributors: R. Graziose*, P. Rojas-Silva *, * , C. Dekock*, M. Grace n , A. Poulev*, M. Ann Lila n, P. Smith*, I. Raskin *
author keywords: Cornus; Antiplasmodial; Antileishmanial; Malaria; Cytotoxicity; Triterpene; Betulinic acid
MeSH headings : Animals; Antimalarials / isolation & purification; Antimalarials / pharmacology; Cell Line; Cornus / chemistry; Inhibitory Concentration 50; Leishmania / drug effects; Leishmaniasis / drug therapy; Muscle, Skeletal / drug effects; Myoblasts / drug effects; Phytotherapy; Plant Bark; Plant Extracts / chemistry; Plant Extracts / pharmacology; Plant Extracts / therapeutic use; Plasmodium falciparum / drug effects; Rats; Trypanocidal Agents / isolation & purification; Trypanocidal Agents / pharmacology; Trypanocidal Agents / therapeutic use
TL;DR:
The compounds isolated in this study, while displaying moderate in vitro antiplasmodial activity, do not fully support the historical importance of C. florida as an antimalarial remedy in North America.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science
Added: August 6, 2018
2011 journal article
Akt-Dependent Anabolic Activity of Natural and Synthetic Brassinosteroids in Rat Skeletal Muscle Cells
Journal of Medicinal Chemistry, 54(12), 4057–4066.
Contributors: D. Esposito* , * , A. Poulev*, S. Komarnytsky* & I. Raskin *
MeSH headings : Anabolic Agents / chemical synthesis; Anabolic Agents / chemistry; Anabolic Agents / pharmacology; Animals; Cell Line; Cell Survival / drug effects; Cholestanones / chemical synthesis; Cholestanones / chemistry; Cholestanones / pharmacology; Mice; Muscle, Skeletal / cytology; Muscle, Skeletal / drug effects; Phosphorylation; Proto-Oncogene Proteins c-akt / metabolism; Rats; Stereoisomerism; Structure-Activity Relationship
TL;DR:
Presence of the 6-keto group in the B ring and stereochemistry of 22α,23α-vicinal hydroxyl groups in the side chain were critical for the anabolic activity, possibly due to higher cytotoxicity of the 22β,23β-hydroxylated brassinosteroids.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger
(Web of Science)
13. Climate Action
(Web of Science)
Sources: ORCID, Web Of Science, Crossref
Added: August 6, 2018
2011 journal article
Antiplasmodial activity of aporphine alkaloids and sesquiterpene lactones from Liriodendron tulipifera L.
JOURNAL OF ETHNOPHARMACOLOGY, 133(1), 26–30.
Contributors: R. Graziose*, * , C. Lategan*, A. Poulev*, P. Smith*, M. Grace n , M. Lila n , I. Raskin *
author keywords: Antimalarial; Aporphine alkaloids; Sesquiterpene lactones; Liriodendron tulipifera L.; Magnoliaceae; Cytotoxicity
MeSH headings : Alkaloids / chemistry; Alkaloids / isolation & purification; Alkaloids / pharmacology; Antimalarials / chemistry; Antimalarials / isolation & purification; Antimalarials / pharmacology; Aporphines / chemistry; Aporphines / isolation & purification; Aporphines / pharmacology; Lactones / chemistry; Lactones / isolation & purification; Lactones / pharmacology; Liriodendron / chemistry; Malaria / drug therapy; Phytotherapy; Plant Bark; Plant Extracts / chemistry; Plant Extracts / isolation & purification; Plant Extracts / pharmacology; Plant Leaves; Sesquiterpenes / chemistry; Sesquiterpenes / isolation & purification; Sesquiterpenes / pharmacology; United States
TL;DR:
This work supports the historical use of Liriodendron tulipifera as an antimalarial remedy of the United States and characterizes its antiplasmodial constituents.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: ORCID, Web Of Science
Added: August 6, 2018
2011 journal article
Design and evaluation of buccoadhesive bi-layer tablet of atenolol
International Journal of Research in Pharmaceutical Sciences, 2(2), 100–103. http://www.scopus.com/inward/record.url?eid=2-s2.0-79955369086&partnerID=MN8TOARS
Contributors: K. Panneer, S. Ramkanth, R. Thirumurugan, K. Kumar & S. Raji
Source: ORCID
Added: July 16, 2022
2007 journal article
Antimycobacterial activity of novel 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(sub)phenyl/pyridylthiourea compounds endowed with high activity toward multidrug-resistant Mycobacterium tuberculosis
J Antimicrob Chemother, 59(6), 1194–1196.
Contributors: D. Sriram *, P. Yogeeswari *, M. Dinakaran* & R. Thirumurugan *
author keywords: antimycobacterial activity; antitubercular activity; thiourea derivatives; oxazole derivatives
MeSH headings : Animals; Antitubercular Agents / chemical synthesis; Antitubercular Agents / pharmacology; Antitubercular Agents / toxicity; Cell Survival / drug effects; Chlorocebus aethiops; Drug Resistance, Multiple, Bacterial / drug effects; Female; Isoniazid / pharmacology; Magnetic Resonance Spectroscopy; Mice; Microbial Sensitivity Tests; Mycobacterium tuberculosis / drug effects; Pyridines / chemical synthesis; Pyridines / pharmacology; Pyridines / toxicity; Structure-Activity Relationship; Tetrazolium Salts; Thiazoles; Thiourea / analogs & derivatives; Thiourea / chemical synthesis; Thiourea / pharmacology; Thiourea / toxicity; Tuberculosis / drug therapy; Tuberculosis / microbiology; Vero Cells
TL;DR:
15 new 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(2'-trifluoromethyl)phenylthiourea compounds were synthesized and found to be the most active, with an in vitro MIC of 0.14 microM and was 80 times more active than isoniazid against MTB and MDR-TB, respectively.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2006 journal article
2,4-Dimethoxyphenylsemicarbazones with anticonvulsant activity against three animal models of seizures: synthesis and pharmacological evaluation
Bioorg Med Chem, 14(9), 3106–3112.
Contributors: R. Thirumurugan *, D. Sriram *, A. Saxena*, J. Stables & P. Yogeeswari *
author keywords: aryl semicarbazones; anticonvulsant; 2,4-dimethoxy; GABA
MeSH headings : Animals; Anticonvulsants / chemical synthesis; Anticonvulsants / chemistry; Anticonvulsants / pharmacology; Central Nervous System / drug effects; Central Nervous System / metabolism; Disease Models, Animal; Male; Mice; Molecular Structure; Oxygen / chemistry; Rats; Seizures / metabolism; Seizures / prevention & control; Semicarbazones / chemical synthesis; Semicarbazones / chemistry; Semicarbazones / pharmacology; Structure-Activity Relationship; gamma-Aminobutyric Acid / metabolism
TL;DR:
N1-(2,4-dimethoxyphenyl)-N4-(propan-2-one)semicarbazone (17) emerged as the most active compound with no neurotoxicity and were found to elevate gamma-aminobutyric acid levels in the midbrain and medulla oblongata regions equipotent to clobazam.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2006 journal article
Discovery of new antitubercular oxazolyl thiosemicarbazones
J Med Chem, 49(12), 3448–3450.
Contributors: D. Sriram *, P. Yogeeswari *, R. Thirumurugan * & R. Pavana *
MeSH headings : Antibiotics, Antitubercular / chemical synthesis; Antibiotics, Antitubercular / chemistry; Antibiotics, Antitubercular / pharmacology; Drug Resistance, Multiple, Bacterial; Microbial Sensitivity Tests; Mycobacterium tuberculosis / drug effects; Structure-Activity Relationship; Thiosemicarbazones / chemical synthesis; Thiosemicarbazones / chemistry; Thiosemicarbazones / pharmacology
TL;DR:
N-(5-cyclobutyl-1,3-oxazol-2-yl)thiosemicarbazone 6q was found to be the most active compound in vitro with minimum inhibitory concentration of 0.05 microg/mL against MTB and MDR-TB and in the in vivo animal model 6q decreased the bacterial load in lung and spleen tissues with 2.1 log 10 protections.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2006 journal article
Epibatidine and its analogues as nicotinic acetylcholine receptor agonist: an update
Nat Prod Res, 20(5), 497–505.
Contributors: P. Yogeeswari *, D. Sriram *, T. Ratan Bal* & R. Thirumurugan *
author keywords: epibatidine; nicotinic acetylcholine receptor; analgesics; alkaloid
MeSH headings : Analgesics, Non-Narcotic / chemistry; Analgesics, Non-Narcotic / pharmacology; Analgesics, Non-Narcotic / therapeutic use; Analgesics, Non-Narcotic / toxicity; Animals; Anura; Bridged Bicyclo Compounds, Heterocyclic / chemistry; Bridged Bicyclo Compounds, Heterocyclic / pharmacology; Bridged Bicyclo Compounds, Heterocyclic / therapeutic use; Bridged Bicyclo Compounds, Heterocyclic / toxicity; Nicotinic Agonists / chemistry; Nicotinic Agonists / pharmacology; Nicotinic Agonists / therapeutic use; Nicotinic Agonists / toxicity; Pain / drug therapy; Phytotherapy; Pyridines / chemistry; Pyridines / pharmacology; Pyridines / therapeutic use; Pyridines / toxicity; Receptors, Nicotinic / drug effects; Skin / metabolism; Structure-Activity Relationship
TL;DR:
An alkaloid isolated from the skin of the Ecuadorian poison frog, Epipedobates tricolor, has attracted attention because of its exceptionally powerful analgesic properties, and the fact that it acts at nicotine rather than opiate receptors.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2006 journal article
Synthesis and structure-activity relationship on anticonvulsant aryl semicarbazones
Medicinal Chemistry, 2(1), 55–62.
Contributors: P. Yogeeswari *, J. Ragavendran*, R. Thirumurugan, S. Induja*, D. Sriram * & J. Stables*
MeSH headings : Animals; Anticonvulsants / administration & dosage; Anticonvulsants / chemical synthesis; Anticonvulsants / therapeutic use; Binding Sites; Electroshock; Injections, Subcutaneous; Mice; Pentylenetetrazole / administration & dosage; Rats; Seizures / chemically induced; Seizures / drug therapy; Semicarbazones / administration & dosage; Semicarbazones / chemical synthesis; Semicarbazones / therapeutic use; Structure-Activity Relationship
TL;DR:
The 4-fluorophenyl substituted semicarbazones (5a-5y) emerged as the most potent compounds exhibiting anticonvulsant activity in mouse intraperitoneal (i.p.) and rat per oral (p.o.) MES, scPTZ and psychomotor seizure screens.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2006 journal article
Synthesis of N4-(2,4-dimethylphenyl) semicarbazones as 4-aminobutyrate aminotransferase inhibitors
Acta Pharm, 56(3), 259–272. http://www.scopus.com/inward/record.url?eid=2-s2.0-33748855540&partnerID=MN8TOARS
Contributors: P. Yogeeswari, D. Sriram, R. Thirumurugan, L. Jeewanlal, S. Jit, J. Ragavendran, R. Kavya, K. Rakhra, V. Saraswat
Source: ORCID
Added: December 9, 2019
2005 journal article
Camptothecin and its analogues: a review on their chemotherapeutic potential
Nat Prod Res, 19(4), 393–412.
Contributors: D. Sriram, P. Yogeeswari, R. Thirumurugan & T. Bal
author keywords: camptothecin; anticancer; topoisomerase I inhibitors
MeSH headings : Animals; Antineoplastic Agents, Phytogenic / chemistry; Antineoplastic Agents, Phytogenic / pharmacology; Camptothecin / analogs & derivatives; Camptothecin / chemistry; Camptothecin / pharmacology; Humans; Molecular Structure; Structure-Activity Relationship
TL;DR:
The phytochemical aspect, and various structural modifications are comprehensively reviewed as in rings A, B, C, D and E of camptothecin.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2005 journal article
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design
J Med Chem, 48(20), 6202–6211.
Contributors: P. Yogeeswari *, D. Sriram *, R. Thirumurugan *, J. Raghavendran*, K. Sudhan*, R. Pavana*, J. Stables*
MeSH headings : 4-Aminobutyrate Transaminase / antagonists & inhibitors; Animals; Anticonvulsants / chemical synthesis; Anticonvulsants / pharmacology; Anticonvulsants / toxicity; Benzamides / chemical synthesis; Benzamides / pharmacology; Benzamides / toxicity; Chemical and Drug Induced Liver Injury / etiology; Drug Design; Female; Male; Mice; Models, Molecular; Motor Activity / drug effects; Rats; Seizures / drug therapy; Seizures / etiology; Semicarbazones / chemical synthesis; Semicarbazones / pharmacology; Semicarbazones / toxicity; Structure-Activity Relationship; gamma-Aminobutyric Acid / blood
TL;DR:
Compound N1-(2,6-dimethylphenyl)-N4-(2-hydroxybenzaldehyde) semicarbazone emerged as a prototype with wide spectrum anticonvulsant agent active in five models of seizure with no neurotoxicity and hepatotoxicity.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2005 journal article
Synthesis of aryl semicarbazones as potential anticonvulsant agents
Biomed Pharmacother, 59(1-2), 51–55.
Contributors: P. Yogeeswari *, D. Sriram *, V. Veena *, R. Kavya *, K. Rakhra*, J. Ragavendran*, S. Mehta*, R. Thirumurugan *, J. Stables*
author keywords: anticonvulsant; aryl semicarbazones; neurotoxicity
MeSH headings : Animals; Anticonvulsants / chemical synthesis; Anticonvulsants / pharmacology; Anticonvulsants / therapeutic use; Brain / drug effects; Brain / metabolism; Electroshock / methods; Male; Mice; Rats; Rats, Sprague-Dawley; Seizures / drug therapy; Seizures / metabolism; Semicarbazones / chemical synthesis; Semicarbazones / pharmacology; Semicarbazones / therapeutic use
TL;DR:
Among the compounds tested, compounds except 3, 4 and 10 showed protection from seizures in both the animal models, and compounds 6 and 8 were found to increase gamma-aminobutyric acid levels in the medulla oblongata region of the rat brain.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2004 journal article
3-Chloro-2-methylphenyl-substituted semicarbazones: synthesis and anticonvulsant activity
Eur J Med Chem, 39(8), 729–734.
Contributors: P. Yogeeswari *, R. Thirumurugan *, R. Kavya *, J. Samuel, J. Stables & D. Sriram *
author keywords: aryl semicarbazones; 3-Chloro-2-methyl substituted phenyl semicarbazones; anti convulsants; CNS depressants
MeSH headings : Animals; Anticonvulsants / chemical synthesis; Anticonvulsants / therapeutic use; Male; Mice; Rats; Rats, Sprague-Dawley; Rats, Wistar; Seizures / prevention & control; Semicarbazones / chemical synthesis; Semicarbazones / therapeutic use
TL;DR:
A series of 3-chloro-2-methylphenyl substituted semicarbazones was synthesized and evaluated for anticonvulsant and CNS activities and exhibited lesser CNS depression and neurotoxicity compared to phenytoin or carbamazepine as was evident from the CNS studies.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
2004 journal article
Antituberculous activity of some aryl semicarbazone derivatives
Bioorg Med Chem Lett, 14(15), 3923–3924.
Contributors: D. Sriram *, P. Yogeeswari * & R. Thirumurugan *
author keywords: antitubercular; aryl semicarbazones
MeSH headings : Antitubercular Agents / chemical synthesis; Antitubercular Agents / pharmacology; Microbial Sensitivity Tests; Molecular Conformation; Molecular Structure; Mycobacterium tuberculosis / drug effects; Semicarbazones / chemical synthesis; Semicarbazones / pharmacology; Structure-Activity Relationship
TL;DR:
This paper is first of its kind in which aryl semicarbazones are reported to possess antimycobacterials potency greater than p-aminosalicylic acid, ethionamide, ethambutol, ciprofloxacin and kanamycin.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2004 journal article
Ion channels as important targets for antiepileptic drug design
Current Drug Targets, 5(7), 589–602.
Contributors: P. Yogeeswari *, J. Ragavendran, R. Thirumurugan *, A. Saxena & D. Sriram*
author keywords: epilepsy; voltage-gated ion channels; antiepileptic drugs; sodium ion channel; calcium ion channel; potassium ion channel; H-channels
MeSH headings : Anticonvulsants / chemistry; Anticonvulsants / pharmacology; Anticonvulsants / therapeutic use; Calcium Channels / drug effects; Calcium Channels / physiology; Chemistry, Pharmaceutical; Epilepsy / drug therapy; Epilepsy / metabolism; Humans; Ion Channels / drug effects; Ion Channels / physiology; Potassium Channels / drug effects; Potassium Channels / physiology; Sodium Channels / drug effects; Sodium Channels / physiology
TL;DR:
A review on the antiepileptic drugs, both established and currently under development targeted to the ion channels in order to bring about effective seizure control is covered.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: December 9, 2019
2003 journal article
Synthesis and anticonvulsant and neurotoxicity evaluation of N <sup>4</sup>-phthalimido phenyl (thio) semicarbazides
European Journal of Pharmaceutical Sciences, 20(3), 341–346.
Contributors: P. Yogeeswari *, D. Sriram *, V. Saraswat *, J. Ragavendran*, M. Kumar *, S. Murugesan*, R. Thirumurugan *, J. Stables
author keywords: phthalimides; semicarbazides; thiosemicarbazides; anticonvulsants; CNS depressants
MeSH headings : Animals; Anticonvulsants / chemical synthesis; Anticonvulsants / therapeutic use; Anticonvulsants / toxicity; Drug Evaluation, Preclinical / methods; Male; Mice; Rats; Rats, Sprague-Dawley; Seizures / drug therapy; Semicarbazides / chemical synthesis; Semicarbazides / toxicity
TL;DR:
The phenyl (thio) semicarbazide derivatives of phthalimido pharmacophore were synthesized and evaluated for their anticonvulsant and neurotoxic properties and exhibited CNS depression and behavioral despair side effects, lesser than the conventional antiepileptic drugs.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(OpenAlex)
Source: ORCID
Added: July 16, 2022
2003 journal article
Synthesis and anticonvulsant and neurotoxicity evaluation of N4-phthalimido phenyl (thio) semicarbazides
Eur J Pharm Sci, 20(3), 341–346.
Contributors: P. Yogeeswari, D. Sriram, V. Saraswat, J. Ragavendran, M. Kumar, S. Murugesan, R. Thirumurugan, J. Stables
Source: ORCID
Added: December 9, 2019
2003 journal article
Synthesis of novel aryl semicarbazones as anticonvulsants with GABA-mediated mechanism
Medicinal Chemistry Research, 12(2), 57–68. http://www.scopus.com/inward/record.url?eid=2-s2.0-0347380971&partnerID=MN8TOARS
Contributors: P. Yogeeswari, D. Sriram, A. Brahmandam, I. Sridharan, R. Thirumurugan & J. Stables
Source: ORCID
Added: July 16, 2022
2000 journal article
Antitumour activity of Rhinacanthone against Dalton's ascitic lymphoma
Biological and Pharmaceutical Bulletin, 23(12), 1438–1440.
Contributors: R. Thirumurugan, S. Kavimani & R. Srivastava
MeSH headings : Animals; Antineoplastic Agents, Phytogenic / pharmacology; Ascitic Fluid / pathology; Benzopyrans / pharmacology; Lymphoma / drug therapy; Lymphoma / pathology; Male; Mice; Naphthoquinones / pharmacology; Neoplasm Transplantation; Plant Extracts / pharmacology; Plants, Medicinal / chemistry; Tumor Cells, Cultured
TL;DR:
After 14 d of inoculation, Rhinacanthone was able to reverse the changes in the haemotological parameters, protein and packed cellular volume consequent to tumour inoculation.
(via Semantic Scholar)
Source: ORCID
Added: December 9, 2019
Employment
Updated: December 19th, 2016 12:44
2016 - present
North Carolina State University Kannapolis, NC, US
Postdoctoral Research Scholar
Plants for Human Health Institute, CALS
2012 - 2017
International Medical University Kuala Lumpur, Wilayah Persekutuan, MY
Assistant Professor
Pharmaceutical Chemistry
2007 - 2012
Rutgers The State University of New Jersey New Brunswick, NJ, US
PostDoc
Plant Biology and Pathology
2006 - 2007
Nycomed Pharma Private Ltd Mumbai, Maharashtra, IN
Research Scientist
Lead Optimization
2005 - 2006
GVK Biosciences Private Limited Hyderabad, Telangana, IN
Senior Research Associate
Medicinal Chemistry
2004 - present
Jubilant Chemsys Limited Noida, Uttar Pradesh, IN
Junior Research Scientist
Medicinal Chemistry - CRO
2000 - 2001
Sami Labs Ltd Bangalore, Karnataka, IN
Research Chemist
Natural Products
Education
Updated: December 19th, 2016 13:01
2011 - 2015
Birla Institute of Technology and Science Pilani, Rajasthan, IN
PhD
School of Pharmacy
1998 - 2000
Banaras Hindu University Varanasi, Uttar Pradesh, IN
MPharmacy
Department of Pharmaceutics
1993 - 1997
Madurai Medical College Madurai, Tamil Nadu, IN
BPharmacy
School of Pharmacy
Funding History
Funding history based on the linked ORCID record. Updated: May 5th, 2016 07:12
grant
January 1, 2015 - December 1, 2016
Efficacy of Andrographis paniculata in preventing the systemic inflammation, metabolic dysfunction and atherosclerosis induced by cholesterol-enriched high-fat diet in animal models
Ministry of Agriculture and Agro based Industry, Malaysia
grant
July 1, 2014 - June 1, 2016
Swietenine, a natural wonder drug, potentiates the antidiabetic activity of metformin: Identification of molecular mechanisms involved
Ministry of Higher Education, Malaysia
grant
July 1, 2014 - December 1, 2016
Identification of chemical probes with pancreatic β-cell-selective replication promoting activity: The new paradigm in anti-diabetic drug discovery
Ministry of Higher Education, Malaysia
grant
June 1, 2013
Structure-based Optimisation of the novel lead compound Tetrahydrothiazolopyridine for the treatment of obesity: Design and synthesis of drug-like compounds; evaluation of their efficacy and toxicity in vivo
Ministry of Higher Education, Malaysia
grant
January 1, 2010 - December 1, 2012
Artemisia Species and Insulin Signaling
National Center for Complementary and Alternative Medicine
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