Basic Information
ID: ALA2439948
Journal: ACS Med Chem Lett
Title: Discovery of DF-461, a Potent Squalene Synthase Inhibitor.
Authors: Ichikawa M, Ohtsuka M, Ohki H, Ota M, Haginoya N, Itoh M, Shibata Y, Ishigai Y, Terayama K, Kanda A, Sugita K.
Abstract: We report the development of a new trifluoromethyltriazolobenzoxazepine series of squalene synthase inhibitors. Structure-activity studies and pharmacokinetics optimization on this series led to the identification of compound 23 (DF-461), which exhibited potent squalene synthase inhibitory activity, high hepatic selectivity, excellent rat hepatic cholesterol synthesis inhibitory activity, and plasma lipid lowering efficacy in nonrodent repeated dose studies.
CiteXplore: 24900587
DOI: 10.1021/ml400151c
Patent ID: ┄
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