Answers are grounded in this paper and cite their sources.
Demonstrates oral efficacy of a novel factor Xa inhibitor in a canine thrombosis model, highlighting non-canonical S1 subsite binding.
The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloaromatic bound in the S(1) subsite. The most potent azaindole, 33 (RPR209685), is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound 33 was efficacious in the canine AV model of thrombosis.
No takes yet. Share an insight, caveat, or question.
Choi-Sledeski et al. (2003) studied this question.
Synapse has enriched 10 related papers. Consider them for comparative context: