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.

中文翻译：

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N-取代的3,5-二苯基-2-吡唑啉衍生物作为环氧合酶（COX-2）抑制剂的合成及生物学评价

已经合成了18种新的1-N-取代的3,5-二苯基-2-吡唑啉衍生物，并评估了环加氧酶（COX-1和COX-2）的抑制活性。这些生物测定的结果表明，所有新衍生物均未具有改善的抗COX-1的抗炎活性，但其中一些具有良好的抗COX-2活性。为了评估最重要的化合物（2d，2f，2g和2k）的结合模式，进行了对接研究。这些研究证实了生物学数据，实际上这些化合物能够适应COX-2的活性位点。