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 oropropionylamino)-1,3,4-t hiadiazole-5-sulfonamide (1); chloroacetylamino)-1,3,4-thiadiazole-5-s ulfonamide (2); and nylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibition effects of these compounds on carbonic anhydrase I an d II have been investigated. By comparing I-50 and K-i values of the c ompounds, it has been found that compound 1 is a more potent inhibitor than acetazolamide (b) on carbonic anhydrase II. (C) 1997 Elsevier Sc ience Ltd.