
Bioorganic and Medicinal Chemistry Letters p. 1667 - 1670 (2002)
Update date:2022-07-30
Topics:
Czekaj, Mark
Klein, Scott I.
Guertin, Kevin R.
Gardner, Charles J.
Zulli, Allison L.
Pauls, Henry W.
Spada, Alfred P.
Cheney, Daniel L.
Brown, Karen D.
Colussi, Dennis J.
Chu, Valeria
Leadley, Robert J.
Dunwiddie, Christopher T.
A systematic modification of the C3 side-chain of the β-aminoester class of factor Xa inhibitors and a survey of P4 variations is described. These changes have resulted in the identification of sub-nanomolar inhibitors with improved selectivity versus related proteases. Coagulation parameters (i.e., APTT doubling concentrations) are also improved.
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