1-(2-萘基)-1H-吡唑-5-甲酰胺作为有效的凝血因子Xa抑制剂。第3部分：口服生物利用度良好的苯甲脒-P4抑制剂的设计、合成及构效关系
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
作者信息
Jia Zhaozhong J, Wu Yanhong, Huang Wenrong, Zhang Penglie, Song Yonghong, Woolfrey John, Sinha Uma, Arfsten Ann E, Edwards Susan T, Hutchaleelaha Athiwat, Hollennbach Stanley J, Lambing Joseph L, Scarborough Robert M, Zhu Bing-Yan
机构信息
Millennium Pharmaceuticals Inc., 256 East Grand Avenue, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1229-34. doi: 10.1016/j.bmcl.2003.12.054.
Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro anticoagulant activity. These benzamidine-P4 fXa inhibitors have displayed excellent oral bioavailability and long half-life.
使用N，N-二烷基化苯甲脒作为新型P4基序，我们设计并合成了一类1-（2-萘基）-1H-吡唑-5-甲酰胺，作为高效且选择性的凝血因子Xa（fXa）抑制剂，其亲水性和体外抗凝血活性得到显著改善。这些苯甲脒-P4 fXa抑制剂表现出优异的口服生物利用度和长半衰期。
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