These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.
    Author: Yoshikawa K, Yoshino T, Yokomizo Y, Uoto K, Naito H, Kawakami K, Mochizuki A, Nagata T, Suzuki M, Kanno H, Takemura M, Ohta T.
    Journal: Bioorg Med Chem Lett; 2011 Apr 01; 21(7):2133-40. PubMed ID: 21345673.
    Abstract:
    We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the identification of compound 30 h which showed both good in vitro activity (fXa IC(50) = 2.2 nM, PTCT2 = 3.9 μM) and in vivo antithrombotic efficacy.
    [Abstract] [Full Text] [Related] [New Search]