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  • Title: Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.
    Author: Nagata T, Yoshino T, Haginoya N, Yoshikawa K, Isobe Y, Furugohri T, Kanno H.
    Journal: Bioorg Med Chem Lett; 2007 Aug 15; 17(16):4683-8. PubMed ID: 17555959.
    Abstract:
    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.
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