Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives.
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Chimenti F, Carradori S, Secci D, Bolasco A, Bizzarri B, Chimenti P, Granese A, Yanez M, Orallo F
Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives.
Eur J Med Chem. 2010 Feb;45(2):800-4. doi: 10.1016/j.ejmech.2009.11.003. Epub 2009 Nov 6.
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- 19926363 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Clorgiline Amine oxidase [flavin-containing] A IC 50 (nM) 4.46 N/A N/A Details Iproniazid Amine oxidase [flavin-containing] B IC 50 (nM) 7540 N/A N/A Details Isatin Amine oxidase [flavin-containing] B IC 50 (nM) 18750 N/A N/A Details Moclobemide Amine oxidase [flavin-containing] A IC 50 (nM) 361380 N/A N/A Details Selegiline Amine oxidase [flavin-containing] A IC 50 (nM) 67250 N/A N/A Details Selegiline Amine oxidase [flavin-containing] B IC 50 (nM) 19600 N/A N/A Details