Aultz D E, Helsley G C, Hoffman D, McFadden A R
J Med Chem. 1977 Jan;20(1):66-70. doi: 10.1021/jm00211a013.
A series of 6,11-dihydrodibenz[b,e]oxepin-2-acetic acids has been evaluated for both antiinflammatory and analgetic activity in the carrageenan paw edema and phenylquinone writhing assays. The requirements for optimal activity in this series appear rather specific: (a) an unsubstituted 6,11-dihydrodibenz[b,e]oxepin nucleus and (b) a carbonyl group in the 11 position. One derivative, 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid (11), has been selected for further study.
在角叉菜胶致爪肿胀和苯醌扭体试验中,对一系列6,11 - 二氢二苯并[b,e]氧杂卓 - 2 - 乙酸进行了抗炎和镇痛活性评估。该系列中最佳活性的要求似乎相当明确:(a) 一个未取代的6,11 - 二氢二苯并[b,e]氧杂卓核;(b) 11位上有一个羰基。已选择一种衍生物,即6,11 - 二氢 - 11 - 氧代二苯并[b,e]氧杂卓 - 2 - 乙酸(11)进行进一步研究。