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Molecules 2015, 20(9), 16221-16234; doi:10.3390/molecules200916221

Synthesis, Biological Evaluation and Molecular Docking Studies of Piperidinylpiperidines and Spirochromanones Possessing Quinoline Moieties as Acetyl-CoA Carboxylase Inhibitors

Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, School of Pharmacy, Xuzhou Medical College, Xuzhou 221004, Jiangsu, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 11 August 2015 / Revised: 30 August 2015 / Accepted: 1 September 2015 / Published: 7 September 2015
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Acetyl-coenzyme A carboxylases (ACCs) play critical roles in the regulation of fatty acid metabolism and have been targeted for the development of drugs against obesity, diabetes and other metabolic diseases. Two series of compounds possessing quinoline moieties were designed, synthesized and evaluated for their potential to inhibit acetyl-CoA carboxylases. Most compounds showed moderate to good ACC inhibitory activities and compound 7a possessed the most potent biological activities against ACC1 and ACC2, with IC50 values of 189 nM and 172 nM, respectively, comparable to the positive control. Docking simulation was performed to position compound 7a into the active site of ACC to determine a probable binding model. View Full-Text
Keywords: acetyl-CoA carboxylase; inhibitors; piperidinylpiperidines; spirochromanones; synthesis; molecular docking acetyl-CoA carboxylase; inhibitors; piperidinylpiperidines; spirochromanones; synthesis; molecular docking
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Huang, T.; Sun, J.; Wang, Q.; Gao, J.; Liu, Y. Synthesis, Biological Evaluation and Molecular Docking Studies of Piperidinylpiperidines and Spirochromanones Possessing Quinoline Moieties as Acetyl-CoA Carboxylase Inhibitors. Molecules 2015, 20, 16221-16234.

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