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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities of some new 2-((2,6-dichloroanilino) phenyl)acetic acid derivatives.
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Synthesis and anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities of some new 2-((2,6-dichloroanilino) phenyl)acetic acid derivatives.

机译：一些新的2-（（（2,6-二氯苯胺基）苯基）乙酸衍生物的合成及抗炎，止痛，促溃疡和脂质过氧化活性。

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摘要

The synthesis of a group of 1,3,4-oxadiazoles, 1,2,4-triazoles, 1,3,4-thiadiazoles and 1,2,4-triazine derived from 2-[(2,6-dichloroanilino) phenyl] acetic acid is described. The structures of new compounds are supported by IR, (1)H-NMR and Mass spectral data. These compounds were tested in vivo for their anti-inflammatory activity. The compounds, which showed activity comparable to the standard drug diclofenac, were screened for their analgesic, ulcerogenic and lipid peroxidation activities. Ten new compounds, out of 28 showed very good anti-inflammatory activity in the carrageenin induced rat paw edema test, with significant analgesic activity in the acetic acid induced writhing test together with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde content (MDA), which is one of the byproduct of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from our results that their protective effects may be related to inhibition of lipid peroxidation in the gastric mucosa.
机译：由2-[（2,6-二氯苯胺基）苯基衍生的一组1,3,4-恶二唑，1,2,4-三唑，1,3,4-噻二唑和1,2,4-三嗪的合成描述了乙酸。 IR，（1）H-NMR和质谱数据支持了新化合物的结构。在体内测试了这些化合物的抗炎活性。筛选出具有与标准药物双氯芬酸相当的活性的化合物的镇痛，促溃疡和脂质过氧化活性。 28种化合物中的10种新化合物在角叉菜胶诱导的大鼠爪水肿试验中显示出非常好的抗炎活性，在乙酸诱导的扭体试验中具有显着的止痛活性，而致溃疡作用却可以忽略不计。这些化合物显示出较少的致溃疡作用，还显示出丙二醛含量（MDA）降低，丙二醛含量是脂质过氧化作用的副产物之一。研究表明，这些化合物抑制了胃粘膜病变的诱导，从我们的结果可以看出，它们的保护作用可能与抑制胃粘膜脂质过氧化有关。

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