Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors
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- 作者：Rossella Fioravanti ; Adriana Bolasco ; Fedele Manna ; Francesca Rossi ; Francisco Orallo ; Matilde Yá ; ñ ; ez ; Alberto Vitali ; Francesco Ortuso ; Stefano Alcaro
- 关键词：Prenylated pyrazoline ; 4 ; 5-Dihydro-(1H)-pyrazole ; hMAO-B inhibitors ; Docking
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 November 2010
- 年：2010
- 卷：20
- 期：22
- 页码：6479-6482
- 全文大小：362 K
文摘
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.