Amir Mohd, Shikha Kumar
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi 110062, India.
Eur J Med Chem. 2004 Jun;39(6):535-45. doi: 10.1016/j.ejmech.2004.02.008.
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.
描述了一组由2-[(2,6-二氯苯胺基)苯基]乙酸衍生的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。新化合物的结构由红外光谱、¹H-NMR和质谱数据证实。这些化合物在体内进行了抗炎活性测试。对显示出与标准药物双氯芬酸相当活性的化合物进行了镇痛、致溃疡和脂质过氧化活性筛选。在28种化合物中,有10种在角叉菜胶诱导的大鼠足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著的镇痛活性,同时致溃疡作用可忽略不计。致溃疡作用较小的化合物也显示出丙二醛含量(MDA)降低,丙二醛是脂质过氧化的副产物之一。研究表明,这些化合物抑制胃黏膜损伤的诱导,从我们的结果可以推测,它们的保护作用可能与抑制胃黏膜中的脂质过氧化有关。