A Medical Approach to the Monoamine Oxidase Inhibition by Using 7Hbenzo[ e]perimidin-7-one Derivatives

Author(s): Mitchell Bacho, Eduardo Coelho-Cerqueira, Cristian Follmer, Seyed Mohammad Nabavi, Luca Rastrelli, Eugenio Uriarte, Eduardo Sobarzo-Sanchez

Journal Name: Current Topics in Medicinal Chemistry

Volume 17 , Issue 4 , 2017

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Graphical Abstract:


Background: A series of perimidinone derivatives (7H-benzo[e]perimidin-7-one) were synthesized and assessed by means of in vitro assays as human MAO inhibitors. These compounds inhibited reversibly the enzymes with inhibitory constants in the range of 2 to 20 μM. In addition, the selectivity of inhibition of the MAO isoforms seems to be significantly dependent of the presence either of heteroatom or electron donating and withdrawing groups on the perimidinone framework, which was verified by using molecular docking simulation with the crystallized MAO receptors. Most of these inhibitors were highly selective: 9 and 11 inhibited selectively the MAO-B isoform while 12 had 10-fold selectivity for MAO-A isoform. Moreover, the compound 12 was both the most selective and potent MAO-A inhibitor among perimidinones.

Result: These results have important implications for the drug design of molecules targeting depression and movement-related disorders.

Keywords: Monoamine oxidase (MAO), 7H-benzo[e]perimidin-7-one, Perimidinones, MAO-A, Anti-Parkinson.

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Article Details

Year: 2017
Page: [489 - 497]
Pages: 9
DOI: 10.2174/1568026616666160824120929
Price: $65

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