RESUMO

Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.

Assuntos

Acetazolamida/análogos & derivados , Anticonvulsivantes/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Diuréticos/farmacologia , Sulfonamidas/química , Tiadiazóis/farmacologia , Anticonvulsivantes/química , Inibidores da Anidrase Carbônica/química , Diuréticos/química , Humanos , Isoenzimas/antagonistas & inibidores , Tiadiazóis/química