☆ 4.5 Article

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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 20, 期 22, 页码 6479-6482

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2010.09.061

关键词

Prenylated pyrazoline; 4,5-Dihydro-(1H)-pyrazole; hMAO-B inhibitors; Docking

类别

Chemistry, Medicinal Chemistry, Organic

资金

MURST (Italy)
Ministerio de Sanidad y Consumo (Spain) [FISS PI061537]
Conselleria de Innovacion e Industria de la Xunta de Galicia (Spain) [INCI-TE07PXI203039ES, INCITE08E1R203054ES, 08CSA019203PR]
FIRB [RBNE034XSW]

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摘要

A series of N-substituted-3-[(2'-hydroxy-40-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. (C) 2010 Elsevier Ltd. All rights reserved.

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