(4-Piperidinyl)-piperazine: A new platform for acetyl-CoA carboxylase inhibitors

Novel disubstituted (4-piperidinyl)-piperazine derivatives as ACC1/2 non-selective inhibitors were synthesized and evaluated. 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 demonstr...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (23), p.6645-6648
Main Authors: Chonan, Tomomichi, Oi, Takahiro, Yamamoto, Daisuke, Yashiro, Miyoko, Wakasugi, Daisuke, Tanaka, Hiroaki, Ohoka-Sugita, Ayumi, Io, Fusayo, Koretsune, Hiroko, Hiratate, Akira
Format: Article
Language:English
Subjects:
(4-Piperidinyl)-piperazine
Acetyl-CoA carboxylase
Acetyl-CoA Carboxylase - antagonists & inhibitors
Biological and medical sciences
Crystallography, X-Ray
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General and cellular metabolism. Vitamins
Inhibitor
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Piperidines - chemical synthesis
Piperidines - chemistry
Piperidines - pharmacology
Stereoisomerism
Structure-Activity Relationship
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Summary:Novel disubstituted (4-piperidinyl)-piperazine derivatives as ACC1/2 non-selective inhibitors were synthesized and evaluated. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.10.012