Low molecular weight thrombin inhibitors with exce...[Bioorg Med Chem Lett. 2004]

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

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

Morrissette MM, Stauffer KJ, Williams PD, Lyle TA, Vacca JP, Krueger JA, Lewis SD, Lucas BJ, Wong BK, White RB, Miller-Stein C, Lyle EA, Wallace AA, Leonard YM, Welsh DC, Lynch JJ, McMasters 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.

PMID: 15261262 [PubMed - indexed for MEDLINE]

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position. [J Med Chem. 1997]
Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety. [Bioorg Med Chem Lett. 2006]
Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors. [Bioorg Med Chem Lett. 2002]
Progress towards the discovery of orally active thrombin inhibitors. [Curr Med Chem. 1998]
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors. [Bioorg Med Chem Lett. 2000]
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Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.

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