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: Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.
    Author: Nordhoff S, Cerezo-Gálvez S, Deppe H, Hill O, López-Canet M, Rummey C, Thiemann M, Matassa VG, Edwards PJ, Feurer A.
    Journal: Bioorg Med Chem Lett; 2009 Aug 01; 19(15):4201-3. PubMed ID: 19515557.
    Abstract:
    Modifications of DPP-4 inhibitor 5, that was discovered by structure based design, are described and structure-activity relationships discussed. With analogue 7k one of the most potent non-covalent inhibitors of DPP-4 reported to date (IC(50)=0.38nM) was discovered. X-ray structure of inhibitor 7k bound to DPP-4 revealed a hydrogen bonding interaction with Q553. First successful efforts in balancing overall properties, as demonstrated by improved metabolic stability, highlight the potential of this series.
    [Abstract] [Full Text] [Related] [New Search]