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1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors |
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| Authors: | 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 |
| Affiliation: | Millennium Pharmaceuticals Inc., 256 East Grand Avenue, South San Francisco, CA 94080, USA. zjia@portola.com |
| Abstract: | 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. |
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