作者
Asif Husain, Mohammed Ajmal
发表日期
2009/6/1
期刊
Acta pharmaceutica
卷号
59
期号
2
页码范围
223-233
出版商
Hrvatsko farmaceutsko društvo
简介
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) values. 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 significant decrease of ulcerogenic activity.
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