Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 8, Pages 3207-3211Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.01.067
Keywords
Carbonic anhydrase; Phenol; 4,4 '-Biphenyl-1,1 '-diphenol; hCA I; hCA II; Enzyme inhibitor
Funding
- Scientific and Technological Research Council of Turkey [TBAG-HD107T882]
- EU
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The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II, with a series of phenol derivatives was investigated by using the esterase assay, with 4- nitrophenyl acetate as substrate. 2,6-Dimethylphenol, 2,6-diisopropylphenol ( propofol), 2,6-di-t-butylphenol, butylated hydroxytoluene, butylated hydroxyanisole, vanillin, guaiacol, di(2,6-dimethylphenol), di( 2,6-diisopropylphenol), di( 2,6-di- t-butylphenol), and acetazolamide showed K-I values in the range of 37.5-274.5 mu M for hCA I and of 0.29 - 113.5 mu M against hCA II, respectively. All these phenols were non-competitive inhibitors with 4- nitrophenylacetate as substrate. Some antioxidant phenol derivatives investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms which have not been yet assayed for their interactions with such agents. (C) 2009 Elsevier Ltd. All rights reserved.
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