CARBONIC-ANHYDRASE ACTIVATORS .14. SYNTHESES OF MONO AND BIS PYRIDINIUM SALT DERIVATIVES OF 2-AMINO-5-(2-AMINOETHYL)-1,3,4-THIADIAZOLE AND 2-AMINO-5-(3-AMINOPROPYL)-1,3,4-THIADIAZOLE AND THEIR INTERACTION WITHISOZYME II

Reaction of 2-amino-5-(2-aminoethyl)- and 2-amino-5-(3-aminopropyl)-1, 3,4-thiadiazole with 2,4,6-trisubstituted pyrylium salts in molar rati os of 1:1 and 1:2 afforded three series of derivatives which were inve stigated for their abilities to activate the enzyme carbonic anhydrase (CA). Only compounds possessing free aminoalkyl moieties behaved as s trong CA II activators, presumably via a mechanism involving the shutt ling of protons between the enzyme active site and the environment.