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  • Title: Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.
    Author: Mochizuki A, Nakamoto Y, Naito H, Uoto K, Ohta T.
    Journal: Bioorg Med Chem Lett; 2008 Jan 15; 18(2):782-7. PubMed ID: 18039572.
    Abstract:
    Previously, we identified cyclohexane diamine derivative 1 as orally bioavailable factor Xa inhibitor. We have investigated two racemic cis-piperidine diamine derivatives 2 and 3 based on 1. Compounds 2a-e showed higher fXa inhibitory activity, anticoagulant activity, and aqueous solubility than 3a-e having same substituent. Compounds 2a, 2c, 2e, and 2g-m having sp2 nitrogen, especially amide and urea derivatives, showed potent anticoagulant activity. Compounds 2h and 2k showed high oral activities in rats.
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