Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur 413 255, Maharashtra, India.
Bioorg Med Chem Lett. 2012 Sep 15;22(18):5839-44. doi: 10.1016/j.bmcl.2012.07.080. Epub 2012 Jul 31.
A novel series of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines (5a-o) has been synthesized and the structures of newly synthesized compounds were characterized by IR, (1)H NMR and mass spectral analysis. All the synthesized compounds were evaluated for their in vitro and in vivo anti-inflammatory activity, and also for their antioxidant activity. Compounds 5b, 5c, 5d and 5n were found to be selective COX-2 inhibitors. Compound 5c was found to potent inhibitor of the carrageenin induced paw edema in rats. Most of the compounds exhibited good DPPH and superoxide radical scavenging activity, while compounds 5c, 5d, 5i and 5k exhibited good hydroxyl radical scavenging activity. Molecular docking result, along with the biological assay data, suggested that compound 5c was a potential anti-inflammatory agent.
已经合成了一系列新型的 3-(取代基)-芳基-5-(9-甲基-3-咔唑基)-1H-2-吡唑啉（5a-o），并通过红外光谱、（1）H NMR 和质谱分析对新合成的化合物的结构进行了表征。所有合成的化合物都进行了体外和体内抗炎活性评估，以及抗氧化活性评估。化合物 5b、5c、5d 和 5n 被发现是选择性 COX-2 抑制剂。化合物 5c 被发现是大鼠角叉菜胶诱导足肿胀的有效抑制剂。大多数化合物表现出良好的 DPPH 和超氧自由基清除活性，而化合物 5c、5d、5i 和 5k 则表现出良好的羟基自由基清除活性。分子对接结果与生物测定数据表明，化合物 5c 是一种有潜力的抗炎药物。
