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Pyrazole carboxylic acid derivatives of 5-amino-1,3,4-thiadiazole-2- sulfonamide (inhibitor 1) were synthesized from ethyl 3-(chlorocarbonyl)-1-(3- nitrophenyl)-5-phenyl-1H-pyrazole-4-carboxylate compound. The inhibitory effects of inhibitor 1, acetazolamide (AAZ) and of 11 newly synthesized amides (5a-b, 6, 7a-g, and 8) on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA-I and hCA-II) have been studied in vitro. The comparison of newly synthesized amides to inhibitor 1 and to AAZ indicated that the new derivatives inhibit CA isoenzymes and they are more potent inhibitors than the parent inhibitor 1 and AAZ. (copyright) 2010 Elsevier Masson SAS. All rights reserved.
R. Kasmoullar. Department of Chemistry, Faculty of Arts and Sciences, Dumlupinar University, Tavanl yolu 10 km, 43100 Kutahya, Turkey. rahmikasimoglu@hotmail.com
3.8 Pharmacology (Part of: 3 Laboratory methods)
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)