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