Synthesis and characterization of some novel 1,3,4-oxadiazole for anti-inflammatory activity

Sarita Chaurasia, Gaddi Divija, Dyapa Divya, M. Divya, H. -, M. Harshitha
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Abstract

A series of five-membered heterocyclic rings were synthesized by the reaction between 2[(4-chlorophenyl) acetyl] benzoic acid and and SOCl2 produced acid chloride and the acid chloride on reaction with substituted aromatic acid to form (3a- 3d) compounds and was tested for their anti-inflammatory activity determined by rat-paw-oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and Mass spectral data. The compounds were purified by column chromatography. All synthesized derivatives were determined by the carrageenan-induced rat-paw-oedema model for anti-inflammatory activity. The entire compound gives good response for the anti-inflammatory activity: 2-(4’-Chloro-phenyl)-1-[2-(5”-phenyl-[1, 3, 4] oxadiazol-2-yl) phenyl]-ethanone (3b), and (2-(4’-Chloro-phenyl)-1-{2-[5”-(4-nitrophenyl)-[1, 3, 4] oxadiazol-2-yl]-phenyl}-ethanone) (3c). For this activity, indometacin was used as a standard drug and compared to new synthesized drugs. Some new synthesized drugs have shown better activities for the anti-inflammation.
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新型抗炎活性1,3,4-恶二唑的合成与表征
用2[(4-氯苯基)乙酰基]苯甲酸与SOCl2反应合成一系列五元杂环,生成氯化酸,氯化酸与取代芳香酸反应生成(3a- 3d)化合物,并采用大鼠脚掌水肿法测定其抗炎活性。所有合成的化合物都通过1HNMR, IR和质谱数据进行了表征。化合物经柱层析纯化。所有合成的衍生物均采用卡拉胶诱导大鼠爪水肿模型进行抗炎活性测定。整个化合物具有良好的抗炎活性:2-(4′-氯苯基)-1-[2-(5′-苯基)-[1,3,4]恶二唑-2-基)苯基]-乙烷酮(3b)和(2-(4′-氯苯基)-1-{2-[5′-(4-硝基)-[1,3,4]恶二唑-2-基]-苯基}-乙烷酮(3c)。以吲哚美辛为标准药物,并与新合成药物进行比较。一些新的合成药物已显示出较好的抗炎活性。
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