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

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