Abstract
A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain.
MeSH terms
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ATP Citrate (pro-S)-Lyase / antagonists & inhibitors*
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Adipose Tissue / drug effects
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Animals
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Anti-Obesity Agents / chemical synthesis
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Anti-Obesity Agents / chemistry*
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Anti-Obesity Agents / pharmacology*
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Benzene / chemistry*
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Blood Glucose / analysis
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Body Weight / drug effects
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Cells, Cultured
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Cholesterol / blood
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Mice
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Rats
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
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Triglycerides / blood
Substances
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Anti-Obesity Agents
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Blood Glucose
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Enzyme Inhibitors
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Sulfonamides
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Triglycerides
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Cholesterol
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ATP Citrate (pro-S)-Lyase
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Benzene