Sparatore F, Savelli F, Cordella G
Farmaco Sci. 1980 Sep;35(9):735-51.
In order to investigate the effects of the overlapping of cinchophene and phenothiazine structures, connected with antiinflammatory and analgesic activities, several derivatives of 2-phenothiazin-2'-yl-cinchoninic acid were prepared through the condensation of isatin or 5-substituted isatins with 2-acetylphenothiazine or its 10-ter-aminoalkyl derivatives. Most of these compounds exhibit analgesic activity, but only a few, of those so far tested, show antiinflammatory activity. Compound (G) with R' = H, R" = C2H5 and R"' = dimethylaminoethyl shows analgesic activity corresponding to 88% of that of phenylbutazone. Moreover some compounds show signs of sympatholytic and vasodilatatory activities and also bactericidal and amebicidal properties in vitro, while some others demonstrate a modest neuroplegic activity.
为了研究与抗炎和镇痛活性相关的辛可芬和吩噻嗪结构重叠的影响，通过异吲哚酮或5-取代异吲哚酮与2-乙酰基吩噻嗪或其10-叔氨基烷基衍生物缩合制备了几种2-吩噻嗪-2'-基喹哪啶酸衍生物。这些化合物大多具有镇痛活性，但到目前为止测试的化合物中只有少数具有抗炎活性。R' = H、R" = C2H5且R"' = 二甲基氨基乙基的化合物(G)的镇痛活性相当于保泰松的88%。此外，一些化合物表现出抗交感神经和血管舒张活性的迹象，并且在体外还具有杀菌和杀阿米巴特性，而其他一些化合物则表现出适度的神经麻痹活性。
