【摘要】 寻找新型潜在的抗炎药物,设计合成系列目标化合物,并测定其抗炎活性。以1H-1,2,4-三唑-3-甲酸甲酯为起始原料,分别与不同取代苯胺经一步反应合成目标化合物,采用鼠耳肿胀法对所合成化合物进行抗炎活性的测定。所有合成化合物结构经1HNMR和13CNMR进行确证,其中N-(4-十二烷氧基苯基)-1H-1,2,4-三唑-3-甲酰胺对小鼠耳肿胀度的抑制率为50.3%,略优于阳性对照药布洛芬(45.6%)。设计合成的目标化合物具有潜在的抗炎活性。更多还原

【Abstract】 Searching for novel potential anti-inflammatory active substances,a series of N-phenyl-1H-1,2,4-triazole-3-carboxamides derivatives were designed,synthesized and evaluated for the anti-inflammatory active.The target compounds of N-(substituted-phenyl)-1H-1,2,4-triazole-3-carboxamides were prepared using methyl 1H-1,2,4-triazole-3-carboxylate and arylamine via one step reaction.The anti-inflammatory activity were investigated by ear swelling model.The structures of synthesized compounds were confirmed by1 HNMR,and the ear tumefaction inhibitory rate of N-(4-(heptyloxy) phenyl)-1H-1,2,4-triazole-3-carboxamide was 50.3%,better than the positive control drug ibuprofen.N-(4-(heptyloxy) phenyl)-1H-1,2,4-triazole-3-carboxamide has been designed and synthesized as potential anti-inflammatory active.更多还原