Document Report Card
Basic Information
ID: ALA1146806
Journal: Bioorg Med Chem Lett
Title: Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Authors: Mederski WW, Dorsch D, Anzali S, Gleitz J, Cezanne B, Tsaklakidis C.
Abstract: Neutral weak halothiophene benzimidazole inhibitors of the serine protease factor Xa were identified via screening of a compound library. The X-ray crystal structure of representative 3a bound to human fXa confirmed the S1 binding mode. Starting from 3a a series of halothiophene benzimidazoles was synthesized and investigated for their factor Xa inhibitory activity. This led to potent and selective achiral inhibitors against fXa such as compounds 9k and 9w.
CiteXplore: 15203158