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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2004.04.097 | DOI Listing |
Publication Analysis
Top Keywords
halothiophene benzimidazoles
8
benzimidazoles surrogates
4
surrogates inhibitors
4
inhibitors blood
4
blood coagulation
4
coagulation factor
4
factor neutral
4
neutral weak
4
weak halothiophene
4
halothiophene benzimidazole
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!