Bioorganic and Medicinal Chemistry Letters p. 3459 - 3464 (1999)
Update date:2022-08-03
Topics:
Ho, Jonathan Z.
Levy, Odile E.
Gibson, Tony S.
Nguyen, Khanh
Semple, J. Edward
A series of novel FXa inhibitors 2a-m and 3a-f was discovered that feature heterocyclic carboxamides tethered to a d-diaminobutyric acid sidechain. These neutral amide derivatives serve as novel P3 d-arginine mimics. Pyrazine carboxamide scaffolds afforded the most potent FXa inhibitors (e.g., 2b IC50 = 4.6 nM). The synthesis and biological activity of two focused libraries are reported.
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