Bioorganic & medicinal chemistry

Inhibitors of the tissue factor/factor VIIa-induced coagulation: synthesis and in vitro evaluation of novel 2-aryl substituted pyrido [3, 4-d][1, 3]-, pyrido [2, 3-d][1, 3]-, …

P Jakobsen, AM Horneman, E Persson

Index: Jakobsen, Palle; Horneman, Anne Marie; Persson, Egon Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 12 p. 2803 - 2812

Full Text: HTML

Citation Number: 32

Abstract

The synthesis of a series of 2-aryl substituted hetero annulated 1, 3-oxazin-4-ones and their evaluation as specific inhibitors of the tissue factor (TF)/factor VIIa (FVIIa)-induced pathway of coagulation is reported. Inhibitory activities (IC50 values) in the range 0.64 to> 40μM on the activation of factor X (FX) by the TF/FVIIa complex were found for compounds having one or two electronegative substituents such as F and NO2 in the 2-aryl substituent. Some of ...