Author/Authors :
Zhaozhong J. Jia، نويسنده , , Yanhong Wu، نويسنده , , Wenrong Huang، نويسنده , , Penglie Zhang، نويسنده , , Yonghong Song، نويسنده , , John Woolfrey، نويسنده , , Uma Sinha، نويسنده , , Ann E. Arfsten، نويسنده , , Susan T. Edwards، نويسنده , , Athiwat Hutchaleelaha، نويسنده , , Stanley J. Hollennbach، نويسنده , , Joseph L. Lambing، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
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.
Keywords :
Factor Xa inhibitors.* Corresponding authors. Tel.: +1-650-246-7073 , fax: +1-650-246-7776 (Z.J.J.) , e-mail: zjia@portola. , tel.: +1-510-402-4032 (B.-Y.Z.)
