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一些具有镇痛和抗炎活性的新型2(3H)-苯并恶唑酮的合成与表征

Synthesis and characterization of some new 2(3H)-benzoxazolones with analgesic and antiinflammatory activities.

作者信息

Gökhan-Kelekçi Nesrin, Köksal Meriç, Unüvar Songül, Aktay Göknur, Erdoğan Hakki

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2009 Feb;24(1):29-37. doi: 10.1080/14756360701841772.

Abstract

The synthesis, characterization and pharmacological activities of a new series of (6-difluorobenzoyl)-5-methyl-3-benzoylmethyl-2(3H)-benzoxazolone and 5-methyl-3-(2-hydroxyl-2-phenylethyl)-2(3H)-benzoxazolone are described. Antiinflammatory activity was investigated by the carrageenin-induced paw oedema test and analgesic activity by acetic acid writhing and hot plate tests in mice. Among the synthesized compounds, compound 3e 6-(2,5-difluorobenzoyl)-3-(4-bromobenzoylmethyl-2(3H)-benzoxazolone was found to be the most promising compound for analgesic activity. Reduced compounds (4a-4d) displayed considerable anti-inflammatory activity compared to the other derivatives.

摘要

描述了一系列新型(6-二氟苯甲酰基)-5-甲基-3-苯甲酰基甲基-2(3H)-苯并恶唑酮和5-甲基-3-(2-羟基-2-苯乙基)-2(3H)-苯并恶唑酮的合成、表征及药理活性。通过角叉菜胶诱导的爪肿胀试验研究抗炎活性,通过小鼠醋酸扭体试验和热板试验研究镇痛活性。在合成的化合物中,化合物3e 6-(2,5-二氟苯甲酰基)-3-(4-溴苯甲酰基甲基)-2(3H)-苯并恶唑酮被发现是镇痛活性最有前景的化合物。与其他衍生物相比,还原后的化合物(4a-4d)表现出相当的抗炎活性。

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