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Bioorg Med Chem Lett. 2002 May 6;12(9):1307-10.

Design and synthesis of aminophenol-based factor Xa inhibitors.

Author information

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

Abstract

A novel potent and selective aminophenol scaffold for fXa inhibitors was developed from a previously reported benzimidazole-based naphthylamidine template. The aminophenol template is more synthetically accessible than the benzimidazole template, which simplified the introduction of carboxylic acid groups. Substitution of a propenyl-para-hydroxy-benzamidine group on the aminophenol template produced selective, sub-nanomolar fXa inhibitors. The potency of the inhibitors is partially explained with the aid of a trypsin complex crystal structure.

PMID:
11965377
DOI:
10.1016/s0960-894x(02)00142-7
[Indexed for MEDLINE]

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