| Literature DB >> 21269824 |
Hans G F Richter1, 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.
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.Entities:
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Year: 2010 PMID： 21269824 DOI： 10.1016/j.bmcl.2010.12.123
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823