Ueno K, Kubo S, Tagawa H, Yoshioka T, Tsukada W
J Med Chem. 1976 Jul;19(7):941-6. doi: 10.1021/jm00229a017.
A series of 6,11-dihydro-11-oxodibenz[b,e]oxepinacetic acids was synthesized and the antiinflammatory activity determined. Studies on 29 compounds revealed certain structure-activity relationships. In the carrageenan edema test, eight compounds exhibited higher antiinflammatory activities than did indomethacin. Several compounds (2, 9, 14, 22, 25) also proved to have activities superior or comparable to indomethacin in suppressing chronic as well as acute inflammation and carrageenan-induced hyperesthesia. Gastric irritation and lethality rates were less frequently observed with these compounds.
合成了一系列6,11 - 二氢 - 11 - 氧代二苯并[b,e]氧杂环庚三烯乙酸,并测定了其抗炎活性。对29种化合物的研究揭示了某些构效关系。在角叉菜胶性水肿试验中,8种化合物表现出比吲哚美辛更高的抗炎活性。几种化合物(2、9、14、22、25)在抑制慢性和急性炎症以及角叉菜胶诱导的感觉过敏方面也被证明具有优于或与吲哚美辛相当的活性。这些化合物较少观察到胃刺激性和致死率。