1291779-96-8Relevant articles and documents
Discovery of BI 99179, a potent and selective inhibitor of type i fatty acid synthase with central exposure
Kley, J?rg T.,MacK, Jürgen,Hamilton, Bradford,Scheuerer, Stefan,Redemann, Norbert
, p. 5924 - 5927 (2011/10/09)
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.