57295-74-6Relevant academic research and scientific papers
HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000363, (2016/05/02)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability
Bali, Ustav,Barba, Oscar,Dawson, Graham,Gattrell, William T.,Horswill, James G.,Pan, David A.,Procter, Martin J.,Rasamison, Chrystelle M.,Sambrook Smith, Colin P.,Taylor-Warne, Amanda,Wong-Kai-In, Philippe
, p. 824 - 828 (2012/03/26)
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.
