Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.

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Fioravanti R, Bolasco A, Manna F, Rossi F, Orallo F, Ortuso F, Alcaro S, Cirilli R

Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.

Eur J Med Chem. 2010 Dec;45(12):6135-8. doi: 10.1016/j.ejmech.2010.10.005. Epub 2010 Oct 25.

PubMed ID
20974503 [ View in PubMed
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Abstract

Eighteen new 1-N-substituted-3,5-diphenyl-2-pyrazoline derivatives have been synthesized and cyclooxygenase (COX-1 and COX-2) inhibitory activities have been evaluated. The results of these biological assays showed that all of new derivatives are not endowed with improved anti-inflammatory activity against COX-1, but some of them showed a good activity against COX-2. To evaluate the binding mode of the most significative compounds (2d, 2f, 2g and 2k) docking studies were carried out. These studies confirmed biological data, in fact these compounds were able to fit into the active site of COX-2.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DiclofenacProstaglandin G/H synthase 2IC 50 (nM)23620N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)35200N/AN/ADetails
NimesulideProstaglandin G/H synthase 2IC 50 (nM)231400N/AN/ADetails