Synthesis,Anti-Inflammatory,and Analgesic Activities of Derivatives of 4-Hydroxy-2-benzoxazolone

Benzoxazolones are widely distributed in plants and are of increasing interest for a variety of pharmacological properties,such as detoxification,antibacterial,anti-inflammatory,and analgesic activities and tranquilizers (michaelidou and hadjipavlou-litina,2005; doʇruer et al.,1998). 4-hydroxy-2-benzoxazolone (hboa) is one of the major bioactive compounds in traditional chinese herb drug acanthus ilicifolius (peng and long,2006) which has obvious anti-inflammatory and analgesic activities (huo et al.,2004; mani senthil kumar et al.,2008; babu et al.,2001). in this research,we used 2-nitroresorcinol as starting material to prepare hboa with a novel one-pot-way. derivatives of hboa tc-2∼tc-4 were obtained via electrophilic reagents and reacted with corresponding primary amines to afford schiff base derivatives tc-5∼tc-10 for further study. anti-inflammatory and analgesic activities of those derivatives were determined by using carrageenan-induced rat paw edema test. the analgesic activities of the derivatives were determined by the hot-plate test. copyright © 2015 guangjin zheng et al.