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    J Med Chem. 2006 Oct 5;49(20):5988-99.

    A novel class of potent nonglycosidic and nonpeptidic pan-selectin inhibitors.

    Ulbrich HK, Luxenburger A, Prech P, Eriksson EE, Soehnlein O, Rotzius P, Lindbom L, Dannhardt G.

    Source

    Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Johannes Gutenberg University, Staudingerweg 5, DE-55099 Mainz, Germany. ulbrich@uni-mainz.de

    Abstract

    An early step of the inflammatory response, the rolling of leukocytes on activated endothelial cells, is mediated by selectin/carbohydrate interactions. The tetrasaccharide sialy Lewisx is a ligand for E-, P-, and L-selectin and therefore serves as a lead structure for the development of analogues. A combination of synthesis and structure-based design allowed rapid optimization. The current lead 2a was evaluated in our E-selectin cell flow chamber assay where it proved to inhibit rolling and adhesion with an IC50 of 28+/-7 microM. The assays used are predictive for the in vivo efficacy of test compounds as shown for 2a in a proteose peptone induced peritonitis model of acute inflammation in mice.

    PMID:
    17004713
    [PubMed - indexed for MEDLINE]

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