Abstract
Inhibitory effects of three new derivatives of 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide on bovine carbonic anhydrase have been investigated. The new compounds are 2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide, 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide, and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide. The new compounds inhibit the esterase activity of carbonic anhydrase noncompetitively and have inhibition constants and I(50) values very similar to those for 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide, the latter being clinically used in the treatment of glaucoma.
MeSH terms
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Acetazolamide / chemistry
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Acetazolamide / pharmacology
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Animals
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Carbonic Anhydrase Inhibitors / chemistry*
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / drug effects
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Cattle
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Drug Evaluation, Preclinical
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Inhibitory Concentration 50
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
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Thiadiazoles / chemistry
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Thiadiazoles / pharmacology
Substances
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2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide
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2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide
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2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide
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Carbonic Anhydrase Inhibitors
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Sulfonamides
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Thiadiazoles
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Carbonic Anhydrases
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Acetazolamide