Abstract
A newly series of water-soluble 1-alkyl-3-(4-methyl-7, 8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride salts (3a-j) were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II from human erythrocytes were purified by a simple one step procedure by using Sepharose 4B-L-tyrosine-sulphanilamide affinity column. The result showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Among them, 3g and 3j were found to be most active (IC(50) = 22.09 µM and 20.33 µM) for hCA I and hCA II, respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / isolation & purification
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Carbonic Anhydrases / metabolism*
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Coumarins / chemical synthesis
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Coumarins / chemistry
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Coumarins / pharmacology*
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Dose-Response Relationship, Drug
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Erythrocytes / enzymology
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Humans
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Molecular Structure
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Protein Isoforms / antagonists & inhibitors
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Protein Isoforms / isolation & purification
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Protein Isoforms / metabolism
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Structure-Activity Relationship
Substances
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Carbonic Anhydrase Inhibitors
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Coumarins
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Protein Isoforms
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coumarin
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Carbonic Anhydrases