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

✍ Scribed by Rossella Fioravanti; Adriana Bolasco; Fedele Manna; Francesca Rossi; Francisco Orallo; Matilde Yáñez; Alberto Vitali; Francesco Ortuso; Stefano Alcaro

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 362 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.09.061

No coin nor oath required. For personal study only.

✦ Synopsis

A series of N-substituted-3-[(2 0 -hydroxy-4 0 -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.

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