Works (4)

Updated: August 2nd, 2023 21:15

2016 journal article

Second generation modifiers of colistin resistance show enhanced activity and lower inherent toxicity

TETRAHEDRON, 72(25), 3549–3553.

By: C. Brackett n, R. Furlani n, R. Anderson n, A. Krishnamurthy n, R. Melander n, S. Moskowitz*, R. Ernst*, C. Melander

author keywords: Antibiotic adjuvant; 2-Aminoimidazole; Colistin; ESKAPE pathogens; Acinetobacter baumannii; Pseudomonas aeruginosa
TL;DR: From these libraries, a new small molecule was identified that lowers the minimum inhibitory concentration of colistin by up to 32-fold greater than the parent compound while also displaying less inherent bacterial effect, thereby minimizing the likelihood of resistance evolution. (via Semantic Scholar)
Source: Web Of Science
Added: August 6, 2018

2015 journal article

Inhibition and breaking of advanced glycation end-products (AGEs) with bis-2-aminoimidazole derivatives

TETRAHEDRON LETTERS, 56(23), 3406–3409.

By: M. Richardson*, R. Furlani n, B. Podell*, D. Ackart*, J. Haugen*, R. Melander n, C. Melander, R. Basaraba*

author keywords: Advanced glycation end-products (AGES); Bis-2-aminoimidazole; Aminoguanidine; Diabetes
TL;DR: The screening of a series of 2-aminoimidazloles for anti-AGE activity is reported, and the identification of a bis-2-aminosidazole lead compound that possesses superior AGE inhibition and breaking activity compared to the known AGE inhibitor aminoguanidine is identified. (via Semantic Scholar)
Source: Web Of Science
Added: August 6, 2018

2015 journal article

Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25(21), 4820–4823.

By: R. Furlani n, M. Richardson*, B. Podell*, D. Ackart*, J. Haugen*, R. Melander n, R. Basaraba*, C. Melander

author keywords: Advanced glycation end-product (AGE); 2-Aminoimidazole; Akabori; Diabetes
MeSH headings : Glycation End Products, Advanced / antagonists & inhibitors; Glycation End Products, Advanced / metabolism; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Molecular Structure; Structure-Activity Relationship
TL;DR: The use of a rapid, scalable, two-step procedure is reported to access a second generation of 2-AI based anti-AGE compounds from commercially available amino acids that exhibit increased AGE inhibition and breaking activty compared to the first generation compounds. (via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being (Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2013 journal article

A flexible approach to 1,4-di-substituted 2-aminoimidazoles that inhibit and disperse biofilms and potentiate the effects of beta-lactams against multi-drug resistant bacteria

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 62, 59–70.

By: R. Furlani n, A. Yeagley n & C. Melander n

author keywords: Biofilms; MRSA; Suppression of antibiotic resistance; 2-Aminoimidazoles
MeSH headings : Biofilms / drug effects; Dose-Response Relationship, Drug; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Molecular Structure; Structure-Activity Relationship; beta-Lactams / chemistry; beta-Lactams / pharmacology
TL;DR: These 2-AITs were found to inhibit biofilm formation by MRSA with low micromolar IC50 values and acted synergistically with oxacillin against MRSA lowering the minimum inhibitory concentration (MIC) 4-fold. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

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