Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P 1 structure–activity relationships of the substituted 1-(2-Naphthyl)-1H- …

…, J Woolfrey, P Wong, B Huang, U Sinha, G Park…

Index: Jia, Zhaozhong J.; Wu, Yanhong; Huang, Wenrong; Goldman, Erick; Zhang, Penglie; Woolfrey, John; Wong, Paul; Huang, Brian; Sinha, Uma; Park, Gary; Reed, Andrea; Scarborough, Robert M.; Zhu, Bing-Yan Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 12 p. 1651 - 1655

Full Text: HTML

Citation Number: 24

Abstract

Based on DuPont Pharmaceuticals' monobenzamidine lead structure SN429, we have designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of non-basic factor Xa inhibitors. We have discovered that the displacement of the benzamidine moiety with substituted 2-naphthyl structures not only results in highly potent factor Xa inhibitors, but also significantly increases their enzyme specificity and oral ...