Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 11, Pages 3977-3981Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm200209n
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Funding
- European Union
- NIH [GM25154]
- Thomas Maren grant
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Aromatic amides comprising branched aliphatic carboxylic acids and 4-aminobenzenesulfonamide were evaluated for their inhibition of carbonic anhydrase (CA) isoforms. Of the most anticonvulsant-active compounds (2, 4, 13, 16, and 17), only 13, 16, and 17 were potent inhibitors of CAs VII and XIV. Compounds 9, 14, and 19 inhibited CA II, while 10 and 12 inhibited all isoforms. Structural studies suggest that differences in the active sites' hydrophobicity modulate the affinity of the inhibitors.
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