Synthesis of novel 1,3,4-oxadiazole derivatives and their biological propertiesReportar como inadecuado

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Acta Pharmaceutica, Vol.59 No.2 June 2009. -

A novel series of 2-3-4-bromophenylpropan-3-one-5-substituted phenyl-1,3,4-oxadiazoles 4a-n have been synthesized from 3-4-bromobenzoylpropionic 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.

1,3,4-oxadiazoles; aroylpropionic acid; anti-inflammatory; analgesic activity; antibacterial activity

Autor: ASIF HUSAIN - ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard Hamdard University, New Delhi-110062,



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