Tert-Butyl 1,5-bis(4-(benzodisothiazol-3-yl)piperazin-1-yl)-1,5- dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent {H} +/{K}+-{ATPase} inhibitors

Sharma, A. and Suhas, R. and Chandana, K. V. and Banu, S. H. and Channe Gowda, D. (2013) Tert-Butyl 1,5-bis(4-(benzodisothiazol-3-yl)piperazin-1-yl)-1,5- dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent {H} +/{K}+-{ATPase} inhibitors. Bioorganic and Medicinal Chemistry Letters, 23 (14). pp. 4096-4098. ISSN 0960-894X

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Official URL: https://doi.org/10.1016/j.bmcl.2013.05.043


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. © 2013 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: article, controlled study, unclassified drug, drug structure, Animals, enzyme inhibition, drug synthesis, in vitro study, Thiazoles, Sheep, Anti-Ulcer Agents, Thiourea, thiourea derivative, urea derivative, omeprazole, proton pump inhibitor, antiulcer activity, spectroscopy, 5 bis4 (benzod]isothiazol 3 yl)piperazin 1 yl] 1, 5 dioxopentan 2 ylcarbamate thiourea derivative, 5 dioxopentan 2 ylcarbamate urea derivative, Carbamates, Gastric Mucosa, Glutamic Acid, H(+)-K(+)-Exchanging ATPase, Proton Pump Inhibitors, tert butyl 1, Urea
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 18 Nov 2019 07:18
Last Modified: 18 Nov 2019 07:18
URI: http://eprints.uni-mysore.ac.in/id/eprint/9585

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