S. Tamura, SEIJI KUZUNA, K. Kawai
Sep 1, 1981
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0
Influential Citations
11
Citations
Quality indicators
Journal
Journal of Pharmacy and Pharmacology
Abstract
The inhibition of prostaglandin (PG) biosynthesis by clidanac (6‐chloro‐5‐cyclohexyl‐1‐indancarboxylic acid, TAI‐284), its metabolites and some analogues has been examined using various microsomal preparations as enzyme source. Clidanac and some analogues were among the most potent inhibitors. The (+)‐isomer of clidanac was shown to be 1000 times more potent than the (−)‐isomer in inhibiting PG synthetase activity. The cis‐3′‐hydroxyl metabolite which retains anti‐inflammatory activity comparable to that of clidanac had much less inhibitory activity. Structure‐activity studies with clidanac analogues showed that the position of halogen substitution in 1‐indancarboxylic acid is of considerable significance for the conformational requirement for binding to the enzyme.