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

Morrissette, Matthew M; Stauffer, Kenneth J; Williams, Peter D; Lyle, Terry A; Vacca, Joseph P; Krueger, Julie A; Lewis, S Dale; Lucas, Bobby J; Wong, Bradley K; White, Rebecca B; Miller-Stein, Cynthia; Lyle, Elizabeth A; Wallace, Audrey A; Leonard, Yvonne M; Welsh, Denise C; Lynch, Joseph J; McMasters, Daniel R

Morrissette, Matthew M; Stauffer, Kenneth J; Williams, Peter D; Lyle, Terry A; Vacca, Joseph P; Krueger, Julie A; Lewis, S Dale; Lucas, Bobby J; Wong, Bradley K; White, Rebecca B; Miller-Stein, Cynthia; Lyle, Elizabeth A; Wallace, Audrey A; Leonard, Yvonne M; Welsh, Denise C; Lynch, Joseph J; McMasters, Daniel R.

Afiliação

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

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

Article em En | MEDLINE | ID: mdl-15261262

ABSTRACT

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.

Assuntos

Antitrombinas/farmacologia; Administração Oral; Antitrombinas/administração & dosagem; Antitrombinas/farmacocinética; Disponibilidade Biológica; Estabilidade de Medicamentos; Peso Molecular

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