| 17555959 |
Nagata T, Yoshino T, Haginoya N, Yoshikawa K, Isobe Y, Furugohri T, Kanno H: Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4683-8. Epub 2007 May 25.
This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane derivative 3j had potent anticoagulant activity as well as anti-fXa activity. Synthetic study of the optical isomers of 3g demonstrated that (-)-3g had more potent activity. |
1(0,0,0,1) |