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Issue 55, 2016, Issue in Progress

Exploring coumarin potentialities: development of new enzymatic inhibitors based on the 6-methyl-3-carboxamidocoumarin scaffold

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Abstract

Novel 6-methyl-3-carboxamidocoumarins (compounds 4–15) were synthesized by an effective three step synthetic strategy and screened towards MAO, AChE and BuChE enzymes. In general, the compounds act as selective MAO-B inhibitors. Compound 11 is highlighted as a potent (IC50 hMAO-B = 4.66 nM), reversible and non-competitive MAO-B inhibitor.

Graphical abstract: Exploring coumarin potentialities: development of new enzymatic inhibitors based on the 6-methyl-3-carboxamidocoumarin scaffold

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Article information


Submitted
28 Feb 2016
Accepted
11 May 2016
First published
12 May 2016

RSC Adv., 2016,6, 49764-49768
Article type
Communication

Exploring coumarin potentialities: development of new enzymatic inhibitors based on the 6-methyl-3-carboxamidocoumarin scaffold

A. Fonseca, M. J. Matos, J. Reis, Y. Duarte, M. Gutiérrez, L. Santana, E. Uriarte and F. Borges, RSC Adv., 2016, 6, 49764 DOI: 10.1039/C6RA05262B

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