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 |
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Authors: | Anamika Sharma R Suhas KV Chandana Syeda Hajira Banu D Channe Gowda |
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Institution: | 1. Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, Karnataka, India;2. Postgraduate Department of Chemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore 570 025, Karnataka, India;3. Postgraduate Department of Biochemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore 570 025, Karnataka, India |
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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. |
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Keywords: | Benzisothiazole Urea Thiourea |
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