期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 23, 期 2, 页码 271-276出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756360701507001
关键词
zonisamide; topiramate; carbonic anhydrase; inhibition; sulfamide; preincubation
Some useful therapeutic agents inhibit certain carbonic anhydrase (CA) isozymes to varying degrees. We have conducted enzyme kinetics studies in a 4-nitrophenyl acetate (4-NPA) hydrolysis assay with the marketed antiepileptic drugs topiramate (1) and zonisamide (2) to determine if their full inhibition of human CA-II and CA-I requires extended preincubation conditions. We found that neither 1 nor 2 requires appreciable preincubation with either enzyme to manifest full inhibitory activity. We also examined the sulfamide cognate of topiramate (3) to characterize its CA inhibitory activity and confirmed that it is a very weak inhibitor, unlike 1 or 2. In a CO2 hydration assay, 3 behaved as a very weak, partial inhibitor of CA-H and CA-I. We conclude that topiramate (1), zonisamide (2), and sulfamide 3 do not require extended exposure to human CA-I or CA-II to manifest full inhibitory activity (4-NPA assay).
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