European Journal of Medicinal Chemistry 2010-01-01

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

Rossella Fioravanti, Adriana Bolasco, Fedele Manna, Francesca Rossi, Francisco Orallo, Francesco Ortuso, Stefano Alcaro, Roberto Cirilli, Rossella Fioravanti, Adriana Bolasco, Fedele Manna, Francesca Rossi, Francisco Orallo, Francesco Ortuso, Stefano Alcaro, Roberto Cirilli

Index: Eur. J. Med. Chem. 45 , 6135-8, (2010)

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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.