Synthesis and investigation of inhibition effects of new carbonic anhydrase inhibitors.
Three new derivatives of 2-substituted 1,3,4-thiadiazole-5-sulfonamide have been synthesized. These compounds are 2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide (1); 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide (2); and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibition effects of these compounds on carbonic anhydrase I and II have been investigated. By comparing I50 and Ki values of the compounds, it has been found that compound 1 is a more potent inhibitor than acetazolamide (b) on carbonic anhydrase II.
Arslan
O
O
Department of Chemistry, Faculty of Science and Arts, Atatürk University, Erzurum, Turkey.
Küfrevioĝlu
O I
OI
Nalbantoĝlu
B
B
D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000378:metabolism; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D007700:Kinetics; D008956:Models, Chemical; D013329:Structure-Activity Relationship
D002257:Carbonic Anhydrase Inhibitors; D002256:Carbonic Anhydrases