Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues
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- 作者：Jennifer X. Qiao ; Xuhong Cheng ; Joanne M. Smallheer ; Robert A. Galemmo ; Spencer Drummond ; Donald J.P. Pinto ; Daniel L. Cheney ; Kan He ; Pancras C. Wong ; Joseph M. Luettgen ; et al.
- 关键词：Factor Xa inhibitors ; Pyrazole-based ; SAR ; N-Arylpiperidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 March 2007
- 年：2007
- 卷：17
- 期：5
- 页码：1432-1437
- 全文大小：414 K
文摘
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.