3q30

Publication Abstract from PubMed

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.

Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.,Ichikawa M, Yokomizo A, Itoh M, Sugita K, Usui H, Shimizu H, Suzuki M, Terayama K, Kanda A Bioorg Med Chem. 2011 Mar 15;19(6):1930-49. Epub 2011 Feb 3. PMID:21353782^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.