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The synthesis and structure–activity relationship of a series of benzenesulfonamide indole inhibitors of cPLA 2 α are described. Substitution of the benzenesulfonamide led to analogues with 50-fold improvement in potency versus the unsubstituted benzenesulfonamide lead compound. Rat pharmacokinetics in a minimal formulation was used to prioritize compounds, leading to the discovery of a potent...
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