tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl) piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K+-ATPase inhibitors

Anamika Sharma, and Suhas, R. and Chandana, K. V. and Syeda Hajira Banu, and Channegowda, D. (2013) tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl) piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K+-ATPase inhibitors. Bioorganic & Medicinal Chemistry Letters, 23 (14). pp. 4096-4098. ISSN 0960-894X

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Official URL: http://dx.doi.org/10.1016/j.bmcl.2013.05.043

Abstract

Amino acids are known to possess variable efficacy against ulceration. Considering the good antiulcer activity of amino acids, a series of urea/thiourea derivatives of glutamic acid conjugated benzisothiazole analogue 3a–u with various substituents on aryl ring were synthesized, spectroscopically characterized and evaluated for in vitro H+/K+-ATPase inhibition. Majority of the compounds possessed potency compared to that of omeprazole, a reference drug. In particular, methoxy derivatives 3p–u were the most active compounds possessing a significant 15-fold increase for para substituent thus, contributing positively to gastric H+/K+-ATPase inhibition.

Item Type: Article
Subjects: Physical Sciences > Chemistry
Divisions: PG Campuses > Manasagangotri, Mysore > Chemistry
Depositing User: Chandrappa
Date Deposited: 27 Jan 2014 05:01
Last Modified: 23 Sep 2015 06:13
URI: http://eprints.uni-mysore.ac.in/id/eprint/16320

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