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; F. Borges

doi:10.1039/c6ra05262b

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, F. Borges

Life Sciences School

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15 Citations (Scopus)

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 (IC₅₀hMAO-B = 4.66 nM), reversible and non-competitive MAO-B inhibitor.

Original language	English
Pages (from-to)	49764-49768
Number of pages	5
Journal	RSC Advances
Volume	6
Issue number	55
DOIs	https://doi.org/10.1039/c6ra05262b
Publication status	Published - 1 Jan 2016

ASJC Scopus subject areas

General Chemistry
General Chemical Engineering

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10.1039/c6ra05262b

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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 (IC50hMAO-B = 4.66 nM), reversible and non-competitive MAO-B inhibitor.",

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T2 - Development of new enzymatic inhibitors based on the 6-methyl-3-carboxamidocoumarin scaffold

AU - Fonseca, A.

AU - Matos, M. J.

AU - Reis, J.

AU - Duarte, Y.

AU - Gutiérrez, M.

AU - Santana, L.

AU - Uriarte, E.

AU - Borges, F.

PY - 2016/1/1

Y1 - 2016/1/1

N2 - 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 (IC50hMAO-B = 4.66 nM), reversible and non-competitive MAO-B inhibitor.

AB - 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 (IC50hMAO-B = 4.66 nM), reversible and non-competitive MAO-B inhibitor.

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U2 - 10.1039/c6ra05262b

DO - 10.1039/c6ra05262b

M3 - Article

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JF - RSC Advances

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ER -

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

Abstract

ASJC Scopus subject areas

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