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Molecules 2014, 19(11), 18620-18631; doi:10.3390/molecules191118620

Synthesis and Biological Evaluation of 2-Phenoxyacetamide Analogues, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors

1
Department of General Surgery, Jinhua Central Hospital, Jinhua 321000, China
2
College of Biological and Environmental Engineering, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310014, China
*
Author to whom correspondence should be addressed.
Received: 11 August 2014 / Revised: 6 November 2014 / Accepted: 7 November 2014 / Published: 14 November 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Monoamine oxidases (EC 1.4.3.4; MAOs), a family of FAD-containing enzymes, is an important target for antidepressant drugs. In this paper, a series of 2-phenoxyacetamide analogues were synthesized, and their inhibitory potency towards monoamine oxidases A (MAO-A) and B (MAO-B) were evaluated using enzyme and cancer cell lysate. 2-(4-Methoxyphenoxy)acetamide (compound 12) (SI = 245) and (2-(4-((prop-2-ynylimino)methyl)phenoxy)acetamide (compound 21) (IC50MAO-A = 0.018 μM, IC50MAO-B = 0.07 μM) were successfully identified as the most specific MAO-A inhibitor, and the most potent MAO-A/-B inhibitor, respectively. The inhibitory activities of these two compounds in living cells were also further evaluated utilizing HepG2 and SHSY-5Y cell lysates. View Full-Text
Keywords: monoamine oxidase; inhibitors; phenoxyacetamides; inhibitory activity; cell lysates monoamine oxidase; inhibitors; phenoxyacetamides; inhibitory activity; cell lysates
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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

Shen, W.; Yu, S.; Zhang, J.; Jia, W.; Zhu, Q. Synthesis and Biological Evaluation of 2-Phenoxyacetamide Analogues, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors. Molecules 2014, 19, 18620-18631.

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