Abstract
The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and human serum isozyme VI, with a series of tosylited aromatic amine derivatives was investigated. The K(I) ranges of compounds 1-14 and acetazolamide against hCA I ranged between 1.130 and- 448.2 μM, against hCA II between 0.103 and- 14.3 μM, and against hCA VI ranged between 0.340 and- 42.39 μM. Tosylited aromatic amine derivatives are thus interesting hCA I, II and VI inhibitors, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzenesulfonates / chemical synthesis*
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Benzenesulfonates / chemistry
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Carbonic Anhydrase I / chemistry*
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Carbonic Anhydrase I / isolation & purification
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Carbonic Anhydrase II / chemistry*
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Carbonic Anhydrase II / isolation & purification
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Carbonic Anhydrase Inhibitors / chemical synthesis*
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrases / blood
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Carbonic Anhydrases / chemistry*
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Carbonic Anhydrases / isolation & purification
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Electrophoresis, Polyacrylamide Gel
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Enzyme Assays
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Erythrocytes / chemistry*
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Erythrocytes / enzymology
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Humans
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Kinetics
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Molecular Mimicry
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Molecular Structure
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Structure-Activity Relationship
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Substrate Specificity
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Sulfapyridine / chemistry
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
Substances
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Benzenesulfonates
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Carbonic Anhydrase Inhibitors
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Sulfonamides
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Carbonic Anhydrase I
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Carbonic Anhydrase II
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Carbonic Anhydrases
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carbonic anhydrase VI
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Sulfapyridine