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首页> 外文期刊>Der chemica Sinica >Design, synthesis and biological evaluation of benzoxazole derivatives as new anti-inflammatory agents
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Design, synthesis and biological evaluation of benzoxazole derivatives as new anti-inflammatory agents

机译:新型抗炎剂苯并恶唑衍生物的设计,合成及生物学评价

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New series of N-(5-(5-(Alkylthio)-1,3,4-oxadiazol-2-yl)benzoxazol-2-yl)benzamide derivatives(VI) were synthesized by the reaction of N-(5-(5-mercapto-1,3,4-oxadiazol-2-yl)benzooxazol-2-yl) benzamides with appropriate alkyl halides. The chemical structures of the synthesized compounds were confirmed by means of IR, 1HNMR, Mass spectral analysis. Further, the synthesized compounds (VIa-VIl) were screened for antiinflammatory activity by using Carrageenan-induced paw edema rat model. The results showed that, compounds VId, VIe, VIf and VIh were significantly (p0.0001) reduced the inflammation there by showed a promising anti-inflammatory activity; where as the compound VIb, VIg and VIi moderately reduced the inflammation. The compounds VIa, VIc, VIj, VIk and VIl showed very poor anti-inflammatory activity towards Carrageenan-induced paw edema rat.
机译:通过N-(5-(-(-(5-(5-(5-(Al-ylkylthio))-1,3,4-oxadiazol-2-yl)benzoxazol-2-yl)benzamide衍生物(VI)合成了新的系列5-巯基-1,3,4-恶二唑-2-基)苯并恶唑-2-基苯甲酰胺与适当的烷基卤化物。通过IR,1 HNMR,质谱分析确认了合成化合物的化学结构。此外,通过使用角叉菜胶诱导的爪水肿大鼠模型筛选合成的化合物(VIa-VI1)的抗炎活性。结果表明,化合物VId,VIe,VIf和VIh显着(p <0.0001)通过显示有希望的抗炎活性而减轻了那里的炎症。化合物VIb,VIg和VIi可适度减轻炎症。化合物VIa,VIc,VIj,VIk和VIl对角叉菜胶诱发的爪水肿大鼠显示出非常差的抗炎活性。

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