Issue 55, 2016, Issue in Progress
From the journal:

RSC Advances

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

A. Fonseca,ab   M. J. Matos,a   J. Reis,a   Y. Duarte,c   M. Gutiérrez,c   L. Santana,b   E. Uriarteb  and  F. Borges*a  

* Corresponding authors

a CIQUP/Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Porto, Portugal

b Departamento de Química Orgánica, Faculdade de Farmacia, Universidade de Santiago de Compostela, Santiago de Compostela, Spain

c Laboratorio de Síntesis Orgánica, Instituto de Química de Recursos Naturales Universidad de Talca, Casilla 747, Talca, Chile

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

DOI
https://doi.org/10.1039/C6RA05262B
Article type
Communication
Submitted
28 Feb 2016
Accepted
11 May 2016
First published
12 May 2016

RSC Adv., 2016,6, 49764-49768

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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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