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  • 标题:Synthesis of novel 1,3,4-oxadiazole derivatives and their biological properties
  • 本地全文:下载
  • 作者:ASIF HUSAIN ; MOHAMMED AJMAL
  • 期刊名称:Acta Pharmaceutica
  • 电子版ISSN:1846-9558
  • 出版年度:2009
  • 卷号:59
  • 期号:2
  • 页码:223-233
  • DOI:10.2478/v10007-009-0011-1
  • 语种:English
  • 出版社:Sciendo
  • 摘要:A novel series of 2-[3-(4-bromophenyl)propan-3-one]-5- -(substituted phenyl)-1,3,4-oxadiazoles (4a-n) have been synthesized from 3-(4-bromobenzoyl)propionic acid (3) with the aim to get better anti-inflammatory and analgesic agents with minimum or without side effects (ulcerogenicity).Compound 3 was reacted with several aryl acid hydrazides (2a-n) in phosphorous oxychloride to obtain the title compounds.Structures of the synthesized compounds were supported by means of IR,1H NMR and mass spectroscopy.Title compounds were evaluated for their anti-inflammatory,analgesic,ulcerogenic and antibacterial activities.Antibacterial activity was expressed as the corresponding minimum inhibitory concentration (MIC).A fair number of compounds were found to have significant anti-inflammatory and analgesic activities,while a few compounds showed appreciable antibacterial activity.The newly synthesized compounds showed very low ulcerogenic action.The findings of the present study indicate that cyclization of the carboxylic group of 3 into novel 1,3,4-oxadiazole nucleus resulted in increased anti-inflammatory and analgesic activities with a significant decrease of ulcerogenic activity.
  • 关键词:1;3;4-oxadiazoles;aroylpropionic acid;anti-inflammatory;analgesic activity;antibacterial activity
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