Cerri R, Pau A, Boatto G, Sparatore F, Satta M, Capasso F
Istituto di Analitica Farmaceutica, Università di Sassari.
Farmaco Sci. 1988 Jan;43(1):91-101.
Thirty-four new N-acylderivatives of 7-amino-2,3-polymethyleneinoles (I) and (II) were prepared and tested, together with a few analogues previously obtained, against carrageenan edema in the rat. Several compounds, at a dose of 1 mmole/kg, exhibit good inhibitory activity, that in some cases is superior to that displayed by indomethacin at a dose of 5 mg/kg. With only one exception, activity is confined to compounds of formula (I) and, generally, derivatives of 2,3-hexamethyleneindole are more active than those of lower homologues.
制备并测试了34种新的7-氨基-2,3-聚亚甲基吲哚（I）和（II）的N-酰基衍生物，以及一些先前获得的类似物，用于对抗大鼠角叉菜胶性水肿。几种化合物在1毫摩尔/千克的剂量下表现出良好的抑制活性，在某些情况下优于吲哚美辛在5毫克/千克剂量下的活性。只有一个例外，活性仅限于式（I）的化合物，一般来说，2,3-六亚甲基吲哚的衍生物比低同系物的衍生物更具活性。
