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Bioorg Med Chem Lett. 2002 May 6;12(9):1311-4.

Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.

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1
Medicinal Chemistry, Berlex Biosciences, 15049 San Pablo Avenue, PO Box 4099, 94804-0099, Richmond, CA, USA

Abstract

Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin. Alternatively, replacement of the naphthylamidine with either a biphenylamidine or propenylbenzamidine not only improves fXa potency and selectivity versus thrombin, but selectivity versus trypsin as well.

PMID:
11965378
DOI:
10.1016/s0960-894x(02)00145-2
[Indexed for MEDLINE]

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