Title of article
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors
Author/Authors
Zuchun (Spring) Zhao، نويسنده , , Damian O. Arnaiz، نويسنده , , Brian Griedel، نويسنده , , Steven Sakata، نويسنده , , Jerry L. Dallas، نويسنده , , Marc Whitlow، نويسنده , , Lan Trinh، نويسنده , , Joseph Post، نويسنده , , Amy Liang، نويسنده , , Michael M. Morrissey، نويسنده , , Kenneth J. Shaw، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
963
To page
966
Abstract
Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500–1000-fold selectivity against thrombin and 50–100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong impact on the FXa inhibitory activity. Crystallography studies suggest that the 2-substituent may have a conformational effect favoring the extended binding conformation.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790774
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