330803-51-5Relevant articles and documents
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors
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
, p. 1229 - 1234 (2004)
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.
