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Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors

Authors :
Matilde Yáñez
Stefano Alcaro
Fedele Manna
Adriana Bolasco
Rossella Fioravanti
Francisco Orallo
Francesco Ortuso
Alberto Vitali
Francesca Rossi
Source :
Bioorganic & Medicinal Chemistry Letters. 20:6479-6482
Publication Year :
2010
Publisher :
Elsevier BV, 2010.

Abstract

A series of N-substituted-3-[(2′-hydroxy-4′-prenyloxy)-phenyl]-5-phenyl-4,5-dihydro-(1H)-pyrazolines were synthesized and tested on human monoamine oxidase-A and -B isoforms. Structure–activity relationships and molecular modelling showed that some substitutions, such as benzyloxy or chlorine atom, improve the best interaction with active site of hMAO-B.

Details

ISSN :
0960894X
Volume :
20
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....10a692515f69f79f007be700a3b8423b
Full Text :
https://doi.org/10.1016/j.bmcl.2010.09.061