497863-58-8Relevant academic research and scientific papers
Substituted acrylamides as factor Xa inhibitors: Improving bioavailability by P1 modification
Song, Yonghong,Clizbe, Lane,Bhakta, Chhaya,Teng, Willy,Li, Wenhao,Wong, Paul,Huang, Brian,Sinha, Uma,Park, Gary,Reed, Andrea,Scarborough, Robert M,Zhu, Bing-Yan
, p. 2043 - 2046 (2007/10/03)
To overcome the low bioavailability of our substituted acrylamide P1 benzamidine factor Xa inhibitors reported previously, neutral and less basic groups were used to replace the benzamidine. As a result, a series of P1 aminoisoquinoline substituted acrylamide Xa inhibitors was identified to be potent, selective, and orally bioavailable. Modification of P4 moiety of these compounds further improved their pharmacokinetic properties.
