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Benzbromarone is an inhibitor of the urate anion transporter (IC50 = 0.3 µM for hURAT1) that prevents renal urate resorption.1 It also potently inhibits CYP2C9 (Ki = 20 nM), a major cytochrome P450 enzyme involved in the metabolic clearance of a wide range of therapeutic agents.2 Several analogs of benzabromarone have been developed with varying binding affinities to CYP2C9 in order to study adverse drug-drug interactions.3
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1. Morin (3,5,7,2',4'-
2. Enantioselective synthesis of cyclohepta[b]indoles: Gram-
3. Clinical and toxicological relevance of CYP2C9: Drug-