Design, synthesis and biological activity of YM-60828 derivatives: potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and …

…, K Sato, Y Sakai-Moritani, S Kaku, T Kawasaki…

Index: Hirayama, Fukushi; Koshio, Hiroyuki; Ishihara, Tsukasa; Watanuki, Susumu; Hachiya, Shunichiro; Kaizawa, Hiroyuki; Kuramochi, Takahiro; Katayama, Naoko; Kurihara, Hiroyuki; Taniuchi, Yuta; Sato, Kazuo; Sakai-Moritani, Yumiko; Kaku, Seiji; Kawasaki, Tomihisa; Matsumoto, Yuzo; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 8 p. 2597 - 2610

Full Text: HTML

Citation Number: 28

Abstract

Factor Xa (FXa) is a serine protease which plays a pivotal role in the coagulation cascade. The inhibition of FXa has received great interest as a potential target for the development of new antithrombotic drug. Herein we describe a series of novel 7-amidino-2-naphthoanilide and 7-amidino-2-naphthalensulfonanilide derivatives which are potent FXa inhibitors. These scaffolds are rigid and are allowed to adopt an L-shape conformation which was ...