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

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• 作者：Rossella Fioravanti ; Adriana Bolasco ; Fedele Manna ; Francesca Rossi ; Francisco Orallo ; Francesco Ortuso ; Stefano Alcaro ; Roberto Cirilli
• 关键词：Pyrazoline ; COX inhibitors ; Molecular modeling
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：December 2010
• 年：2010
• 卷：45
• 期：12
• 页码：6135-6138
• 全文大小：376 K

文摘

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.