Author/Authors :
Jennifer X. Qiao، نويسنده , , Xuhong Cheng، نويسنده , , Joanne M. Smallheer، نويسنده , , Robert A. Galemmo Jr.، نويسنده , , Spencer Drummond، نويسنده , , Donald J.P. Pinto، نويسنده , , Daniel L. Cheney، نويسنده , , Kan He، نويسنده , , Pancras C. Wong، نويسنده , , Joseph M. Luettgen، نويسنده , , Robert M. Knabb، نويسنده , , Ruth R. Wexler، نويسنده , , Patrick Y.S. Lam، نويسنده ,
Abstract :
The synthesis, SAR, pharmacokinetic profile, and modeling studies of both monocyclic and fused pyrazoles containing substituted N-arylpiperidinyl P4 moieties that are potent and selective factor Xa inhibitors will be discussed. Fused pyrazole analog 16a, with a 2′-methylsulfonylphenyl piperidine P4 group, was shown to be the best compound in this series (FXa Ki = 0.35 nM) based on potency, selectivity, and pharmacokinetic profile.
Keywords :
Factor Xa inhibitors , Pyrazole-based , SAR , N-Arylpiperidine
