193152-95-3Relevant academic research and scientific papers
Optimization of the β-aminoester class of factor Xa inhibitors. Part 1: P4 and side-chain modifications for improved in vitro potency
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.
, p. 1667 - 1670 (2007/10/03)
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.
