Title of article
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
5
From page
1657
To page
1661
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792282
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