Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595168 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ustav Bali, Oscar Barba, Graham Dawson, William T. Gattrell, James G. Horswill, David A. Pan, Martin J. Procter, Chrystelle M. Rasamison, Colin P. Sambrook Smith, Amanda Taylor-Warne, Philippe Wong-Kai-In,