Title of article
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs
Author/Authors
Penglie Zhang، نويسنده , , Liang Bao، نويسنده , , Jingmei F. Zuckett، نويسنده , , Erick A. Goldman، نويسنده , , Zhaozhong J Jia، نويسنده , , Ann Arfsten، نويسنده , , Susan Edwards، نويسنده , , Uma Sinha، نويسنده , , Athiwat Hutchaleelaha، نويسنده , , Gary Park، نويسنده , , Joseph L Lambing، نويسنده , , Stanley J. Hollenbach، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
983
To page
987
Abstract
Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity were performed at the central phenyl ring and at the S4 binding biphenyl region by incorporating water solublizing substituents. The resulting compounds (e.g., 7, 8, 14, 30a, and 32b) are highly potent in vitro, and show improved activity in human plasma-based thrombin generation assay.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794114
Link To Document