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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4533-9. doi: 10.1016/j.bmcl.2011.05.126. Epub 2011 Jun 17.

Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.

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Boehringer Ingelheim Pharmaceuticals Inc., Medicinal Chemistry, Ridgefield, CT 06877, USA.


A new class of chymase inhibitor featuring a benzimidazolone core with an acid side chain and a P(1) hydrophobic moiety is described. Incubation of the lead compound with GSH resulted in the formation of a GSH conjugate on the benzothiophene P(1) moiety. Replacement of the benzothiophene with different heterocyclic systems such as indoles and benzoisothiazole is feasible. Among the P(1) replacements, benzoisothiazole prevents the formation of GSH conjugate and an in silico analysis of oxidative potentials agreed with the experimental outcome.

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