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首页> 外文期刊>Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry >Synthesis, Characterization, and Biological Evaluation of Novel 3-(4-Chlorophenyl)-2-(substituted)quinazolin-4(3H)-one Derivatives as Multi-target Anti-inflammatory Agents
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Synthesis, Characterization, and Biological Evaluation of Novel 3-(4-Chlorophenyl)-2-(substituted)quinazolin-4(3H)-one Derivatives as Multi-target Anti-inflammatory Agents

机译:新型3-(4-氯苯基)-2-(取代)喹唑啉-4(3H)的合成,表征和生物学评价为多靶抗炎剂的衍生物

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摘要

A novel class of 3-(4-chlorophenyl)-2-(substituted)quinazolin-4(3H)-one derivatives were synthesized, and the structure of synthesized compounds was characterized by IR, H-1 NMR, and mass spectroscopy. The newly synthesized compounds (4a-g and 6a-g) were tested for their in vitro cyclooxygenase (COX) inhibition activity. The compounds have inhibitory profile against both COX-1 and COX-2, and some of the compounds are found to be selective against COX-2. The compound 6g showed distinct inhibitory activity on COXs. The synthesized compounds were evaluated for their potential anti-inflammatory activity as inhibitors of the proinflammatory cytokines IL-6. Compounds 4d-g showed the highest level of inhibition among all the tested compounds. Thus, our data suggested that these compounds may represent a new class of potent anti-inflammatory agents.
机译:合成了一种新型的3-(4-氯苯基)-2-(取代的)喹唑啉-4(3H) - 酮衍生物,并且合成化合物的结构的特征在于IR,H-1 NMR和质谱。 测试新合成的化合物(4A-G和6A-G),用于其体外环氧化酶(COX)抑制活性。 该化合物对COX-1和COX-2具有抑制性曲线,发现一些化合物是针对COX-2的选择性。 化合物6g在COX上显示出明显的抑制活性。 评价合成化合物的潜在抗炎活性作为促炎细胞因子IL-6的抑制剂。 化合物4D-G显示所有测试化合物中的最高抑制水平。 因此,我们的数据表明这些化合物可以代表新类效力的抗炎剂。

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