Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1362178 | Bioorganic & Medicinal Chemistry Letters | 2011 | 7 Pages |
Abstract
Structure-guided lead optimization of recently described benzimidazolyl acetamides addressed the key liabilities of the previous lead compound 1. These efforts culminated in the discovery of 4-{(S)-2-[2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-3-fluoro-benzoic acid 7g, a highly potent and selective FXR agonist with excellent physicochemical and ADME properties and potent lipid lowering activity after oral administration to LDL receptor deficient mice.
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Authors
Hans G.F. Richter, G.M. Benson, K.H. Bleicher, D. Blum, E. Chaput, N. Clemann, S. Feng, C. Gardes, U. Grether, P. Hartman, B. Kuhn, R.E. Martin, J.-M. Plancher, M.G. Rudolph, F. Schuler, S. Taylor,