Abstract
It has been demonstrated that once-a-day dosing of systemically-distributed SCD inhibitors leads to adverse events in eye and skin. Herein, we describe our efforts to convert a novel class of systemically-distributed potent triazole-based uHTS hits into liver-targeted SCD inhibitors as a means to circumvent chronic toxicity.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology*
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Liver / drug effects*
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Liver / enzymology
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Mice
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Rats
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Stearoyl-CoA Desaturase / antagonists & inhibitors*
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Tissue Distribution
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Triazoles / chemistry
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Triazoles / pharmacokinetics
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Triazoles / pharmacology*
Substances
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Enzyme Inhibitors
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Triazoles
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Stearoyl-CoA Desaturase