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 (< 5 µM) more potent than the reference standard, rutin (41.9 µM).
Keywords: Amino acids, piperazine, conjugation, urea/thiourea, antiglycation.
Protein & Peptide Letters
Title:Synthesis and SAR Studies of Urea and Thiourea Derivatives of Gly/Pro Conjugated to Piperazine Analogue as Potential AGE Inhibitors
Volume: 20 Issue: 8
Author(s): Doddahindaiah M. Suyoga Vardhan, Chavalmane S. Shantharam, Ramesh Suhas, Malavalli B. Sridhara and D. Channe Gowda
Affiliation:
Keywords: Amino acids, piperazine, conjugation, urea/thiourea, antiglycation.
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 (< 5 µM) more potent than the reference standard, rutin (41.9 µM).
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Vardhan M. Suyoga Doddahindaiah, Shantharam S. Chavalmane, Suhas Ramesh, Sridhara B. Malavalli and Gowda Channe D., Synthesis and SAR Studies of Urea and Thiourea Derivatives of Gly/Pro Conjugated to Piperazine Analogue as Potential AGE Inhibitors, Protein & Peptide Letters 2013; 20 (8) . https://dx.doi.org/10.2174/0929866511320080005
DOI https://dx.doi.org/10.2174/0929866511320080005 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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