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Bioorg Med Chem Lett. 2004 Aug 16;14(16):4161-4.

Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.

Author information

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

Abstract

Modification of lead compound 1 by reducing lipophilicity in the P3 group produced a series of low molecular weight thrombin inhibitors with excellent potency in functional assays, metabolic stability, and oral bioavailability. These modifications led to the identification of two optimized compounds, 14 and 16.

PMID:
15261262
DOI:
10.1016/j.bmcl.2004.06.030
[Indexed for MEDLINE]

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