Abstract
The discovery, optimization and structure-activity relationship of novel FATP1 inhibitors have been described. The detailed SAR studies of each moiety of the inhibitors combined with metabolite analysis led to the identification of the potent inhibitors 11p and 11q with improved blood stability.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Animals
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Benzoxazoles / chemical synthesis
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Benzoxazoles / chemistry*
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Benzoxazoles / pharmacokinetics
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Drug Evaluation, Preclinical
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Fatty Acid Transport Proteins / antagonists & inhibitors*
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Fatty Acid Transport Proteins / metabolism
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Humans
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Injections, Intravenous
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Mice
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Rats
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Structure-Activity Relationship
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Triazoles / chemical synthesis
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Triazoles / chemistry*
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Triazoles / pharmacokinetics
Substances
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Benzoxazoles
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Fatty Acid Transport Proteins
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N-((4-ethyl-5-(((5-(trifluoromethoxy)-1,3-benzoxazol-2-yl)methyl)sulfanyl)-4H-1,2,4-triazol-3-yl)methyl)aniline
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Triazoles