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首页> 外文期刊>Asian journal of research in chemistry >Synthesis of Some Novel 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives as Potential Antibacterial and Anti-inflammatory activity
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Synthesis of Some Novel 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives as Potential Antibacterial and Anti-inflammatory activity

机译:一些新型的2,5-二取代的1,3,4-恶二唑衍生物的合成具有潜在的抗菌和抗炎活性

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摘要

A novel series of 2-Amidino-5-aryl-1,3,4-oxadiazole derivatives (N2-N4) have been synthesized. A mixture of 2-Amino-5-aryl-1',3,4-oxadiazole, powdered anhydrous aluminium chloride and acetonitrile heated in an oil bath keeping the temperature at 150-160°C for 2 hours to synthesize the derivatives (N1N4). The structures of newly synthesized compourfds were established on die basis of FT- IR, ~1H NMR and Mass spectroscopic techniques, The newly synthesized compounds were screened for their in vitro antibacterial activity and in vivo anti- inflammatory activity. In vitro anti-baeterial activity was evaluated by Disc Diffusion technique against Ofloxacin used as standard drug. In vivo anti-inflammatory activity was determined by (jarageenan Induced Rat Paw Oedema method against Ibuprofen used as standard drug. Compounds Ni and N2 exhibited good antibacterial activity, compound N4 showed moderate antibacterial activity and compound N3 showed poor antibacterial activity. Compound N4 showed good antiinflammatory activity, compounds N1 and N3 showed moderate anti-inflammatory activity and compound N2 showed poor anti-inflammatory activity.
机译:合成了一系列新颖的2-A基-5-芳基-1,3,4-恶二唑衍生物(N2-N4)。将2-氨基-5-芳基-1',3,4-恶二唑,粉末状无水氯化铝和乙腈的混合物在油浴中加热,将温度在150-160°C保持2小时以合成衍生物(N1N4) 。基于FT-IR,〜1H NMR和质谱技术建立了新合成的化合物的结构,并筛选了新合成的化合物的体外抗菌活性和体内抗炎活性。通过圆盘扩散技术评估了氧氟沙星作为标准药物的体外抗细菌活性。以(异黄酮类药物为标准药物,用异黄酮类药物诱导的大鼠爪水肿法)测定体内抗炎活性。化合物Ni和N2显示出良好的抗菌活性,化合物N4显示出中等的抗菌活性,化合物N3显示出较差的抗菌活性。化合物N4显示出良好的抗菌活性。抗炎活性,化合物N1和N3显示中等的抗炎活性,化合物N2显示差的抗炎活性。

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