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

Bioorganic & medicinal chemistry letters 2004 Aug 16; 14(16):4161-4

Link to PubMed abstract

Morrissette M MM, Stauffer K KJ, Williams P PD, Lyle T TA, Vacca J JP, Krueger J JA, Lewis S SD, Lucas B BJ, Wong B BK, White R RB, Miller-Stein C C, Lyle E EA, Wallace A AA, Leonard Y YM, Welsh D DC, Lynch J JJ, McMasters D DR

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

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.