Abstract
Acetyl-CoA carboxylases (ACCs), the rate limiting enzymes in de novo lipid synthesis, play important roles in modulating energy metabolism. The inhibition of ACC has demonstrated promising therapeutic potential for treating obesity and type 2 diabetes mellitus in transgenic mice and preclinical animal models. We describe herein the synthesis and structure-activity relationships of a series of disubstituted (4-piperidinyl)-piperazine derivatives as a new platform for ACC1/2 non-selective inhibitors.
MeSH terms
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Acetyl-CoA Carboxylase / antagonists & inhibitors*
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Crystallography, X-Ray
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Drug Design
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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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Models, Molecular
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Molecular Structure
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Piperazines / chemical synthesis
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Piperazines / chemistry
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Piperazines / pharmacology*
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Piperazines
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Piperidines
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Acetyl-CoA Carboxylase