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Bioorg Med Chem Lett. 2003 Oct 20;13(20):3477-82.

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. ken_rittle@merck.com

Abstract

Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the alpha-thrombin-hirugen complex provides an explanation for these unanticipated results.

PMID:
14505652
DOI:
10.1016/s0960-894x(03)00732-7
[Indexed for MEDLINE]

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