Kataria Aditya Kumar, Khan Suroor Ahmad, Alam Mohammad Mumtaz, Husain Asif, Akhtar Mymoona, Khanna Suruchi, Haider Rashiduddin, Shaquiquzzaman Mohammad
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062, India.
Acta Pol Pharm. 2011 May-Jun;68(3):381-6.
A series of 2-(substituted-phenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazoles (3-15) were synthesized. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. The percentage inhibition in edema at different time intervals indicated that compounds 8, 11, 12, 14 and 15 exhibited good anti-inflammatory potential. The results illustrate that 2-(2-acetoxyphenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazole (15) and 2-(3,4-dimethoxyphenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazole (12) showed best anti-inflammatory activity among the series tested. Furthermore, activity is higher in case of chloro substitution as compared to methyl substitution. The compounds synthesized were also evaluated for their ulcerogenic and lipid peroxidation action and showed superior GI safety profile along with reduction in lipid peroxidation as compared to that of ibuprofen.
合成了一系列2-（取代苯基）-5-（N，N-二苯胺基甲基）-1,3,4-恶二唑（3-15）。对这些化合物的抗炎、镇痛、致溃疡和脂质过氧化作用进行了评估。不同时间间隔的水肿抑制百分比表明，化合物8、11、12、14和15具有良好的抗炎潜力。结果表明，在测试的系列化合物中，2-（2-乙酰氧基苯基）-5-（N，N-二苯胺基甲基）-1,3,4-恶二唑（15）和2-（3,4-二甲氧基苯基）-5-（N，N-二苯胺基甲基）-1,3,4-恶二唑（12）表现出最佳的抗炎活性。此外，与甲基取代相比，氯取代情况下的活性更高。还对合成的化合物的致溃疡和脂质过氧化作用进行了评估，结果显示与布洛芬相比，它们具有更好的胃肠道安全性，同时脂质过氧化作用降低。
