二苯并[b,e]氧杂环庚烷羧酸作为非甾体抗炎药。2. 二氢-10-氧代呋喃并和噻吩并[3,2-c][1]苯并氧杂环庚烷-8-乙酸。
Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 2. Dihydro-10-oxofuro-and -thieno[3,2-c][1]benzoxepin-8-acetic acids.
作者信息
Aultz D E, McFadden A R
出版信息
J Med Chem. 1977 Mar;20(3):456-8. doi: 10.1021/jm00213a028.
PMID:845879
Abstract
4,10-Dihydro-10-oxofuro[3,2-c][1]benzoxepin-8-acetic acid and 4,10-dihydro-10-oxothieno[3,2-c][1]benzoxepin-8-acetic acid were evaluated in the carrageenan paw edema assay with the thieno analogue being ten times more active than the furano compound and 1.3. times more active than indomethacin. The therapeutic ratio (antiinflammatory activity/gastric irritation liability) of the thieno analogue was 25 times that of indomethacin.
摘要
在角叉菜胶致爪肿胀试验中对4,10 - 二氢 - 10 - 氧代呋喃并[3,2 - c][1]苯并氧杂卓 - 8 - 乙酸和4,10 - 二氢 - 10 - 氧代噻吩并[3,2 - c][1]苯并氧杂卓 - 8 - 乙酸进行了评估，结果表明噻吩类似物的活性比呋喃化合物高10倍，比吲哚美辛高1.3倍。噻吩类似物的治疗指数（抗炎活性/胃刺激倾向）是吲哚美辛的25倍。
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