Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Exploring Nitrostyrene as a Scaffold for a New Class a of Monoamine Oxidase Inhibitors

Author(s): Joana Reis, Catarina Oliveira, Nuno Milhazes, Dolores Vina, Fernanda Borges.

Abstract:

With the ultimate purpose of finding out the structural features that are relevant for MAO inhibitory activity and selectivity towards MAO-B isoform, a series of compounds encompassing a β-nitrostyrene moiety was designed and the in vitro inhibitory activity was evaluated. In the present work, we report the synthesis and the pharmacological evaluation of a series of functionalized derivatives of β-methyl-β-nitrostyrene with distinct substitution patterns in the phenyl ring, namely hydroxyl, methoxy, benzyloxy and methylenedioxy. All the studied compounds were substituted in meta and para positions of the phenyl ring related to the nitrovinyl side chain. The synthesized compounds were evaluated towards both human MAO isoforms, displaying some of them activities in the low micromolar range. Particularly compound 6 (a methylenedioxy derivative) exhibits high potency and selectivity towards MAO-B.

Keywords: β-nitrostyrene derivatives, MAO, Neurodegenerative diseases, Monoamine oxidase, metabolism, fluorimetric method, tyramine, Aldrich Química

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Article Details

VOLUME: 9
ISSUE: 10
Year: 2012
Page: [958 - 961]
Pages: 4
DOI: 10.2174/1570180811209050958
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