Format

Send to

Choose Destination
Eur J Med Chem. 2010 Feb;45(2):800-4. doi: 10.1016/j.ejmech.2009.11.003. Epub 2009 Nov 6.

Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives.

Author information

1
Dipartimento di Chimica e Tecnologie del Farmaco, Università di Roma, La Sapienza Ple Aldo Moro 5, 00185 Rome, Italy.

Abstract

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 IC(50) 2.75+/-0.81muM value and selectivity ratio of 25, which is the best candidate for further investigations.

PMID:
19926363
DOI:
10.1016/j.ejmech.2009.11.003
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center