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Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.
MedLine Citation:
PMID:  22217874     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
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
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-12-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2012-1-5     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Prosidion Ltd, Windrush Court, Watlington Road, Oxford, OX4 6LT, United Kingdom.
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