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Bioorg Med Chem Lett
; 22(2): 824-8, 2012 Jan 15.
Article
in English
| MEDLINE
| ID: mdl-22217874
ABSTRACT
A series of potent carboxylic acid DGAT1 inhibitors with high permeability were developed from a virtual screening hit. Strategies were employed to reduce Pgp substrate recognition and increase passive permeability, resulting in the discovery of a series showing good inhibition of cellular triglyceride synthesis. The mutagenic potential of prospective metabolites was evaluated in the Ames assay, and one aniline was shown to be devoid of mutagenicity.