期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 2, 页码 800-804出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.11.003
关键词
Pyrazoline; hMAO inhibitors; Parkinson's disease; N-Thiocarbamoyl
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]
- Conselleria de Educacion y Ordenacion Universitaria de la Xunta de Galicia (Spain)
A series of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives has been synthesized and assayed for their ability to inhibit the activity of the A and B isoforms of human monoamine oxidase (hMAO). Some of these compounds were endowed with a selective inhibitory activity against hMAO-B in the micromolar range. The most active of the series is the compound 13, N1-thiocarbamoyl-3-(fur-2'-yl)-5-(4'-fluoro-phenyl)-4,5-dihydro-(1H)-pyrazole, with IC50 2.75 +/- 0.81 mu M value and selectivity ratio of 25, which is the best candidate for further investigations. (C) 2009 Elsevier Masson SAS. All rights reserved.
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