Kajitani M, Yamazaki T, Yamada S, Tanaka M, Ogawa K, Honna T, Miyake H, Yabuuchi T, Fujimura H
Chemical Synthesis Research Laboratory, Taiho Pharmaceutical Company, Ltd., Saitama, Japan.
Arch Pharm (Weinheim). 1990 Jun;323(6):355-9. doi: 10.1002/ardp.19903230607.
A number of arylbiurets were prepared and evaluated as antiinflammatory and analgesic agents by using the carrageenan paw edema and acetic acid stretching tests. Among them, the antiinflammatory activity of 1,3-dimethyl-5-phenylbiuret (7), 1-ethyl-3-methyl-5-phenylbiuret (11), and 1,1,3-trimethyl-5-phenylbiuret (13) were found to be more potent than phenylbutazone. The analgesic activity of 7 and of 5-(4-chlorophenyl)-1,1,3-trimethylphenylbiuret (16) is higher than that of aminopyrine.
制备了多种芳基缩二脲，并通过角叉菜胶足爪水肿试验和乙酸扭体试验对其作为抗炎和镇痛剂进行了评估。其中，发现1,3 - 二甲基 - 5 - 苯基缩二脲（7）、1 - 乙基 - 3 - 甲基 - 5 - 苯基缩二脲（11）和1,1,3 - 三甲基 - 5 - 苯基缩二脲（13）的抗炎活性比保泰松更强。7和5 -（4 - 氯苯基）- 1,1,3 - 三甲基苯基缩二脲（16）的镇痛活性高于氨基比林。
