Synthesis and evaluation of novel ureido/thioureido derivatives of amino acid conjugated 2,3-dichlorophenyl piperazine as highly potent antiglycating agents

Vardhan,, D. M. Suyoga and Shantharam, C. S. and Suhas, R. and Channe Gowda, D. (2017) Synthesis and evaluation of novel ureido/thioureido derivatives of amino acid conjugated 2,3-dichlorophenyl piperazine as highly potent antiglycating agents. Journal of Saudi Chemical Society, 21. S248 - S257. ISSN 1319-6103

Text (Full Text) Synthesis and evaluation of novel ureidothioureido derivatives of amino acid conjugated 2,3-dichlorophenyl piperazine as highly potent antiglycating agents.pdf - Published Version Restricted to Registered users only Download (1MB) | Request a copy

Abstract

We report the synthesis and in vitro antiglycation activity of more than 80 amino acid–heterocycle conjugate derived ureas and thioureas. They were characterized by physical and spectroscopical methods. Many of the analogues synthesized showed activity at the sub-micro molar level. Introduction of different amino acids as linker and systematic variation of the substituents on the aromatic ring revealed promising leads. In particular, compounds containing Glu and Tyr as the linkers exhibited high antiglycating potency with IC50 1–4μM as against the reference, rutin with IC50 41.9μM. Conclusions Compounds bearing halogen atoms emerged as the most active analogues and serve as lead for future studies.

Item Type:	Article
Uncontrolled Keywords:	Amino acids, Piperazine, Conjugation, Urea/thiourea, Antiglycation
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	C Swapna Library Assistant
Date Deposited:	27 Jun 2019 05:29
Last Modified:	27 Jun 2019 05:29
URI:	http://eprints.uni-mysore.ac.in/id/eprint/3911

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