1,3,4-Thiadiazole-5-sulfonamides as carbonic anhydrase inhibitors: Relationship between their electronic and hydrophobic structures and their inhibitory activity.

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Abstract
Huckel molecular orbital method and Hansch and Fujita''s extrathermodynamic method were employed to characterize the chemical structure of 1,3,4-thiadiazole-5-sulfonamide derivatives which are potent carbonic anhydrase (EC 4.2.1.1) inhibitors. Regression analysis showed that a good correlation exists between the positive charge on nitrogen-10 and the inhibitory activity. The hydrophobicity of the side chain is another factor of development of enzyme inhibition. These results are consistent with the findings of X-ray crystallography.