Synthesis and SAR studies of urea and thiourea derivatives of Gly/Pro conjugated to piperazine analogue as potential AGE inhibitors

Vardhan, D. M. S. and Shantharam, C. S. and Suhas, R. and Sridhara, M. B. and Chenne Gowda, D. (2013) Synthesis and SAR studies of urea and thiourea derivatives of Gly/Pro conjugated to piperazine analogue as potential AGE inhibitors. Protein and Peptide Letters, 20 (8). pp. 888-897. ISSN 0929-8665

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Official URL: http://doi.org/10.2174/0929866511320080005

Abstract

Synthesis of a series of urea and thiourea derivatives of glycine and proline conjugated to 2,3-dichlorophenyl piperazine has been reported. The structures were confirmed by physical and spectroscopical measurements followed by characterization of antiglycation activity. All synthesized compounds were able to inhibit protein glycation, particularly halogen containing derivatives without preference of oxygen or sulphur at the urea function. The best analogues are nearly 20 fold (\textless 5 μM) more potent than the reference standard, rutin (41.9 μM).

Item Type: Article
Uncontrolled Keywords: 3 dichlorophenyl)piperazin 1 yl 2 oxoethylcarbamate]thiourea derivative, 3 dichlorophenyl)piperazin 1 yl 2 oxoethylcarbamate]urea derivative, 3 dichlorophenyl)piperazine 1 carbonyl pyrrolidine 1 carboxylate]thiourea derivative, 3 dichlorophenyl)piperazine 1 carbonyl pyrrolidine 1 carboxylate]urea derivative, Advanced, advanced glycation end product, analogs and derivatives, antagonists and inhibitors, antiglycation activity, article, carbanilamide derivative, chemical structure, chemistry, controlled study, drug activity, drug conjugation, drug determination, drug potency, drug screening, drug structure, drug synthesis, glycine, Glycine, Glycosylation End Products, human, Humans, in vitro study, infrared spectroscopy, Molecular Structure, Phenylurea Compounds, piperazine derivative, Piperazines, proline, Proline, protein glycosylation, proton nuclear magnetic resonance, rutoside, structure activity relation, Structure-Activity Relationship, synthesis, tert butyl 2 4 (2, thiourea, Thiourea, unclassified drug
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 30 Oct 2019 11:24
Last Modified: 06 Jul 2022 07:04
URI: http://eprints.uni-mysore.ac.in/id/eprint/9677

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