Author/Authors :
Penglie Zhang، نويسنده , , Jingmei F. Zuckett، نويسنده , , John Woolfrey، نويسنده , , Katherine Tran، نويسنده , , Brian Huang، نويسنده , , Paul Wong، نويسنده , , Uma Sinha، نويسنده , , Gary Park، نويسنده , , Andrea Reed، نويسنده , , John Malinowski، نويسنده , , Stan Hollenbach، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Abstract :
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.
