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

R Fioravanti, A Bolasco, F Manna, F Rossi…

Index: Fioravanti, Rossella; Bolasco, Adriana; Manna, Fedele; Rossi, Francesca; Orallo, Francisco; Yanez, Matilde; Vitali, Alberto; Ortuso, Francesco; Alcaro, Stefano Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6479 - 6482

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Citation Number: 31

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.