title: 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.
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.
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, Karnataka, India.
authors.forename: Anamika
authors.initials: A
authors.lastname: Sharma
authors.forename: R
authors.initials: R
authors.lastname: Suhas
authors.forename: K V
authors.initials: KV
authors.lastname: Chandana
authors.forename: Syeda Hajira
authors.initials: SH
authors.lastname: Banu
authors.forename: D
authors.initials: D
authors.lastname: Channe Gowda
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002219:Carbamates / Q000737:chemistry*; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D018698:Glutamic Acid / Q000737:chemistry; D017506:H(+)-K(+)-Exchanging ATPase / Q000737:chemistry* / Q000378:metabolism; D054328:Proton Pump Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D012756:Sheep; D013844:Thiazoles / Q000737:chemistry; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014508:Urea / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000897:Anti-Ulcer Agents; D002219:Carbamates; D054328:Proton Pump Inhibitors; D013844:Thiazoles; C466948:benzisothiazole; D018698:Glutamic Acid; D014508:Urea; D017506:H(+)-K(+)-Exchanging ATPase; D013890:Thiourea