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

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

European journal of medicinal chemistry (2010-10-27)
Rossella Fioravanti, Adriana Bolasco, Fedele Manna, Francesca Rossi, Francisco Orallo, Francesco Ortuso, Stefano Alcaro, Roberto Cirilli
要旨

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.

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製品内容

Sigma-Aldrich
インドメタシン, 98.5-100.5% (in accordance with EP)
Sigma-Aldrich
インドメタシン, meets USP testing specifications