Rachlin S, Bramm E, Ahnfelt-Rønne I, Arrigoni-Martelli E
J Med Chem. 1980 Jan;23(1):13-20. doi: 10.1021/jm00175a004.
A variety of basic N,N',N'',-trisubstituted guanidines was prepared and tested for antiinflammatory activity. Compounds with a thiazolylguanidine moiety linked to the 4 position of the 2-methylquinoline ring exhibited fairly high antiinflammatory activity. Optimal activity was associated with the presence of N-cycloalkyl substituents on N''-4-(2-methylquinolyl)-N'-2-thiazolylguanidine. Pharmacological data on N-cyclohexyl-N''-4-(2-methylquinolyl)-N'-2-thiazolylguanidine (SR 1368, 44) are presented and discussed.
制备了多种基本的N,N',N''-三取代胍,并测试了它们的抗炎活性。与2-甲基喹啉环4位相连的噻唑基胍部分的化合物表现出相当高的抗炎活性。最佳活性与N''-4-(2-甲基喹啉基)-N'-2-噻唑基胍上N-环烷基取代基的存在有关。给出并讨论了N-环己基-N''-4-(2-甲基喹啉基)-N'-2-噻唑基胍(SR 1368,44)的药理学数据。