Title of article
Design, synthesis and structure–Activity relationships of benzoxazinone-Based factor Xa inhibitors
Author/Authors
Wenrong Huang، نويسنده , , Penglie Zhang، نويسنده , , Jingmei F. Zuckett، نويسنده , , Lingyan Wang، نويسنده , , John Woolfrey، نويسنده , , Yonghong Song، نويسنده , , Zhaozhong J. Jia، نويسنده , , Lane A. Clizbe، نويسنده , , Ting Su، نويسنده , , Katherine Tran، نويسنده , , Brian Huang، نويسنده , , Paul Wong، نويسنده , , Uma Sinha، نويسنده , , Gary Park، نويسنده , , Andrea Reed، نويسنده , , John Malinowski، نويسنده , , Stanley J. Hollenbach، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
6
From page
561
To page
566
Abstract
A series of benzoxazinone derivatives was designed and synthesized as factor Xa inhibitors. We demonstrated that the naphthyl moiety in the aniline-based compounds 1 and 2 can be replaced with benzene-fused heterobicycles and biaryls to give factor Xa inhibitors with improved trypsin selectivity. The P4 modifications lead to monoamidines which are moderately active. The benzoxazinones 41–45 are potent against factor Xa, retain the improved trypsin selectivity of the corresponding aniline-based compounds, and show strong antithrombotic effect dose responsively.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792966
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