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ID: ALA1833814

Journal: Bioorg Med Chem Lett

Title: Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.

Authors: Kley JT, Mack J, Hamilton B, Scheuerer S, Redemann N.

Abstract: Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats.

CiteXplore: 21873051

DOI: 10.1016/j.bmcl.2011.07.083