Ureas/thioureas of benzodisothiazole analog conjugated glutamic acid: Synthesis and biological evaluation

Sharma, A. and Suhas, R. and Channe Gowda, D. (2013) Ureas/thioureas of benzodisothiazole analog conjugated glutamic acid: Synthesis and biological evaluation. Archiv der Pharmazie, 346 (5). pp. 359-366.

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Official URL: http://doi.org/10.1002/ardp.201200470

Abstract

A series of urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were synthesized, spectroscopically characterized, and evaluated for their in vitro antiglycation and urease inhibitory activities. Preliminary screening of the synthesized compounds 1-35 showed significant results. Amongst these, compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference standards. Hence, they may serve as new lead compounds for further development. Urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were evaluated for their in vitro antiglycation and urease inhibitory activities. Compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference compounds.

Item Type: Article
Uncontrolled Keywords: article, priority journal, drug screening, drug structure, enzyme inhibition, drug synthesis, in vitro study, Structure-Activity Relationship, drug potency, Thiazoles, proton nuclear magnetic resonance, carbon nuclear magnetic resonance, Thiourea, thiourea derivative, urea derivative, glutamic acid, Enzyme Inhibitors, Glutamic Acid, Urea, Advanced, conjugation, Glycosylation End Products, urease, Urease
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 12 Nov 2019 09:20
Last Modified: 18 Nov 2019 07:16
URI: http://eprints.uni-mysore.ac.in/id/eprint/9621

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