6,11-二氢-11-氧代二苯并[b,e]硫代平链烷酸及相关化合物的合成与抗炎活性
Synthesis and antiinflammatory activity of 6,11-dihydro-11-oxodibenzo[b,e]thiepinalkanoic acids and related compounds.
作者信息
Ackrell J, Antonio Y, Franco F, Landeros R, Leon A, Muchowski J M, Maddox M L, Nelson P H, Rooks W H, Roszkowski A P, Wallach M B
出版信息
J Med Chem. 1978 Oct;21(10):1035-44. doi: 10.1021/jm00208a007.
Acetic acid derivatives of tricyclic systems, such as 6,11-dihydro-11-oxodibenzo[b,e]thiepin, 4,10-dihydro-4-oxo-thieno[2,3-c][1]benzothiepin, dibenzo[b,f]thiepin, dibenz[b,f]oxepin, etc., were synthesized and assayed for antiinflammatory activity. One of the compounds, 6,11-dihydro-11-oxodibenzo[b,e]thiepin-3-acetic acid (52), was chosen for evaluation in man on the basis of high antiinflammatory activity in both short- and long-term animal assays and a low gastric irritation liability in rats and dogs.
三环系统的乙酸衍生物，如6,11 - 二氢 - 11 - 氧代二苯并[b,e]硫氮杂蒽、4,10 - 二氢 - 4 - 氧代噻吩并[2,3 - c][1]苯并硫氮杂蒽、二苯并[b,f]硫氮杂蒽、二苯并[b,f]氧杂䓬等，已被合成并测定其抗炎活性。其中一种化合物，6,11 - 二氢 - 11 - 氧代二苯并[b,e]硫氮杂蒽 - 3 - 乙酸（52），基于其在短期和长期动物试验中均具有高抗炎活性以及在大鼠和狗中胃刺激性较低，被选用于人体评估。
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