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Protein & Peptide Letters


ISSN (Print): 0929-8665
ISSN (Online): 1875-5305

Synthesis and SAR Studies of Urea and Thiourea Derivatives of Gly/Pro Conjugated to Piperazine Analogue as Potential AGE Inhibitors

Author(s): Doddahindaiah M. Suyoga Vardhan, Chavalmane S. Shantharam, Ramesh Suhas, Malavalli B. Sridhara and D. Channe Gowda

Volume 20, Issue 8, 2013

Page: [888 - 897] Pages: 10

DOI: 10.2174/0929866511320080005

Price: $65


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.

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