330943-14-1Relevant articles and documents
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors
Zhang, Penglie,Zuckett, Jingmei F.,Woolfrey, John,Tran, Katherine,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stan,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 1657 - 1661 (2007/10/03)
Monoamidine FXa inhibitors 3 were designed and synthesized. SAR studies and molecular modeling led to the design of conformationally constrained diaryl ethers 4 and 5, as well as benzopyrrolidinone 7 as potent FXa inhibitors. The monoamidines show high efficacy in a DVT model, but lack desirable oral bioavailability. The benzopyrrolidinone-based aminoisoquinolines 8 do not show significant improvement in oral bioavailability.
