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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Aroylpropionic acid based 2,5-disubstituted-1,3,4-oxadiazoles: synthesis and their anti-inflammatory and analgesic activities.
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Aroylpropionic acid based 2,5-disubstituted-1,3,4-oxadiazoles: synthesis and their anti-inflammatory and analgesic activities.

机译：基于2,5-二取代-1,3,4-恶二唑的芳酰基丙酸：合成及其抗炎和镇痛活性。

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摘要

Synthesis and biological evaluation of various aroylpropionic acid derivatives containing 1,3,4-Oxadiazole nucleus is reported here. The compounds (3a-w) were synthesized by cyclization of 3-aroylpropionic acids into 1,3,4-oxadiazole nucleus by treating with various aryl acid hydrazides in the presence of POCl(3). The structures of new compounds are supported by IR, (1)H NMR and MS data. These compounds were tested in vivo for their anti-inflammatory activity. All the compounds tested showed anti-inflammatory activity. The compounds which showed activity comparable to the standard drug ibuprofen were screened for their analgesic, ulcerogenic and lipid peroxidation activities. Seven (3c, g, i, j, m, o, p) out of 23 new compounds showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test with very less ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde production (MDA), which is one of the byproducts of lipid peroxidation. Compound 3i and o showed 89.50 and 88.88% of inhibition in paw edema, 69.80 and 66.25% protection against acetic acid induced writhings and 0.7 and 0.65 of severity index respectively, compared to 90.12, 72.50 and 1.95 values of ibuprofen. The study showed that the cyclization of carboxylic group of aroylpropionic acids into an oxadiazole nucleus resulted in compounds having good anti-inflammatory and analgesic effects with reduced gastric irritation.
机译：本文报道了各种含1,3,4-氧杂二唑核的芳酰基丙酸衍生物的合成和生物学评估。通过在POCl（3）存在下用各种芳基酰肼处理，将3-芳基丙酸环化成1,3,4-恶二唑核，合成化合物（3a-w）。新化合物的结构得到IR，（1）H NMR和MS数据的支持。在体内测试了这些化合物的抗炎活性。所有测试的化合物均显示出抗炎活性。筛选显示出与标准布洛芬相当的活性的化合物的镇痛，促溃疡和脂质过氧化活性。 23种新化合物中的7种（3c，g，i，j，m，o，p）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，而致溃疡的作用却非常低。该化合物显示出较少的致溃疡作用，还显示出丙二醛产生减少（MDA），丙二醛是脂质过氧化的副产物之一。化合物3i和o对爪水肿的抑制作用分别为89.50和88.88％，对乙酸引起的扭绞的抑制作用分别为69.80和66.25％，严重度指数分别为90.12、72.50和1.95，而布洛芬的保护作用为90.12、72.50和1.95。研究表明，芳酰基丙酸的羧基环化成恶二唑核可产生具有良好的抗炎和镇痛作用并降低胃部刺激性的化合物。

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