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  • Title: Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.
    Author: Ichikawa M, Yokomizo A, Itoh M, Usui H, Shimizu H, Suzuki M, Terayama K, Kanda A, Sugita K.
    Journal: Bioorg Med Chem; 2011 Mar 15; 19(6):1930-49. PubMed ID: 21353782.
    Abstract:
    To obtain small and efficient squalene synthase inhibitors, a flexible 2-aminobenzhydrol open form structure was designed and showed potent inhibitory activity comparable to 4,1-benzoxazepin compounds. Further chemical modification led to the discovery of a novel template with a strong squalene synthase inhibitory activity, and its basic structure-activity relationship was revealed. The X-ray crystallographic data of compound 12 bound to the active site of squalene synthase provided an important insight into the binding mode of this alternative template that formed 11-membered ring conformations with an intramolecular hydrogen bond.
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