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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis, biological evaluation, and docking studies of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines as potent anti-inflammatory and antioxidant agents
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Synthesis, biological evaluation, and docking studies of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines as potent anti-inflammatory and antioxidant agents

机译:3-(取代)-芳基-5-(9-甲基-3-咔唑)-1H-2-吡唑啉作为有效的抗炎和抗氧化剂的合成,生物学评估和对接研究

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摘要

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, 1H 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.
机译:合成了一系列新的3-(取代)-芳基-5-(9-甲基-3-咔唑)-1H-2-吡唑啉(5a-o),并用IR,1H对新合成的化合物进行了表征NMR和质谱分析。评价所有合成的化合物的体外和体内抗炎活性,以及​​抗氧化活性。发现化合物5b,5c,5d和5n是选择性COX-2抑制剂。发现化合物5c是角叉菜胶诱导的大鼠足水肿的有效抑制剂。大多数化合物表现出良好的DPPH和超氧化物自由基清除活性,而化合物5c,5d,5i和5k表现出良好的羟自由基清除活性。分子对接结果以及生物学测定数据表明,化合物5c是潜在的抗炎药。

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