某些2-芳基-6-苯并恶唑乙酸衍生物的合成与抗炎活性
Synthesis and antiinflammatory activity of some 2-aryl-6-benzoxazoleacetic acid derivatives.
作者信息
Dunwell D W, Evans D
出版信息
J Med Chem. 1977 Jun;20(6):797-801. doi: 10.1021/jm00216a011.
PMID:874954
Abstract
Various approaches to the synthesis of 2-aryl-6-substituted benzoxazoles are described. The products, which included the 6-methyl derivative 4a, ethylamines 10 and 19, ethanols 12 and 14, the acetic and alpha-methylacetic acids 9 and 16a--f, and the acetic ester 11, were screened for antiinflammatory activity on the carrageenan-induced rat paw edema test. Some of the compounds possessed activity superior to that of phenylbutazone and of the same order as that of benoxaprofen.
摘要
描述了合成2-芳基-6-取代苯并恶唑的各种方法。对产物进行了筛选，这些产物包括6-甲基衍生物4a、乙胺10和19、乙醇12和14、乙酸和α-甲基乙酸9和16a - f以及乙酸酯11，通过角叉菜胶诱导的大鼠足爪水肿试验检测其抗炎活性。一些化合物具有优于保泰松的活性，与苯恶洛芬的活性相当。
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