Isoxazolines and isoxazoles as factor Xa inhibitors.

Pruitt, J R; Pinto, D J; Estrella, M J; Bostrom, L L; Knabb, R M; Wong, P C; Wright, M R; Wexler, R R

Pruitt, J R; Pinto, D J; Estrella, M J; Bostrom, L L; Knabb, R M; Wong, P C; Wright, M R; Wexler, R R.

Pruitt JR; The DuPont Pharmaceuticals Company, Wilmington, Delaware 19880-0500, USA. james.r.pruitt@dupontpharma.com

Bioorg Med Chem Lett ; 10(8): 685-9, 2000 Apr 17.

Article en En | MEDLINE | ID: mdl-10782664

RESUMEN

3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency. They were also compared in an arterio-venous (A-V) shunt model of thrombosis.

Asunto(s)

Inhibidores del Factor Xa; Isoxazoles/farmacología; Inhibidores de Serina Proteinasa/farmacología; Animales; Cristalografía por Rayos X; Isoxazoles/química; Isoxazoles/farmacocinética; Modelos Moleculares; Conejos; Inhibidores de Serina Proteinasa/química; Inhibidores de Serina Proteinasa/farmacocinética; Relación Estructura-Actividad; Trombosis/prevención & control

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Banco de datos: MEDLINE Asunto principal: Inhibidores de Serina Proteinasa / Inhibidores del Factor Xa / Isoxazoles Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Año: 2000 Tipo del documento: Article

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