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ID: ALA1938228
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.
Authors: Bali U, Barba O, Dawson G, Gattrell WT, Horswill JG, Pan DA, Procter MJ, Rasamison CM, Sambrook Smith CP, Taylor-Warne A, Wong-Kai-In P.
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.
CiteXplore: 22217874