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Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO ‐ B Inhibitors
Author(s) -
MoralesCamilo Nicole,
Salas Cristian O.,
Sanhueza Claudia,
EspinosaBustos Christian,
SepúlvedaBoza Silvia,
ReyesParada Miguel,
GonzalezNilo Fernando,
CaroliRezende Marcos,
Fierro Angélica
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12458
Subject(s) - chemistry , monoamine oxidase , monoamine oxidase b , stereochemistry , chalcone , in vitro , docking (animal) , biochemistry , enzyme , combinatorial chemistry , medicine , nursing
A series of chalcones and aurones were synthesized and evaluated in vitro as monoamine oxidase inhibitors ( MAO i). Our results show that aurones, which had not been previously reported as MAO i, are MAO ‐B inhibitors. Thus, both families inhibited selectively the B isoform of MAO in the micromolar range, offering novel scaffolds for the design of new and potent MAO inhibitors. The main structural requirements for their activity were characterized with the aid of 3D‐ QSAR and docking studies.