Design and synthesis of amino acids-conjugated heterocycle derived ureas/thioureas as potent inhibitors of protein glycation

Shantharam, C. S. and Suyoga Vardhan, D. M. and Suhas, R. and Channe Gowda, D. (2014) Design and synthesis of amino acids-conjugated heterocycle derived ureas/thioureas as potent inhibitors of protein glycation. Russian Journal of Bioorganic Chemistry, 40 (4). pp. 443-454. ISSN 1608-330X

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Abstract

Protein glycation is believed to play an important role in the development of long-term disorders associated with diabetic complications. In view of the wide occurrence of advanced glycation end products (AGE's) and the oxidative stress derived from them in a variety of diabetic complications, it would be of great interest to identify and develop AGE inhibitors. In this study, synthesis and in vitro antiglycation activity of a small library of forty urea/thiourea derivatives of Phe/Tyr/Glu/Lys-benzisoxazole hybrids are reported. Structures of the compounds were confirmed by IR, NMR, mass spectrometry, and elemental analysis. Most of the title compounds exhibited promising activity. Best antiglycation activity was found for Tyr analogue with methoxy group as a substituent particularly at the para position with IC50 value of 1.9 μM against the positive control, Rutin, with IC50 = 41.9 μM. Thus, the title compounds represent novel class of potent antiglycating agents.

Item Type:	Article
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	20 Aug 2019 07:47
Last Modified:	20 Aug 2019 07:47
URI:	http://eprints.uni-mysore.ac.in/id/eprint/4400

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