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

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).

Cite this article as:

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