Klioze S S, Ehrgott F J, Wilker J C, Woodward D L
J Med Chem. 1979 Dec;22(12):1497-504. doi: 10.1021/jm00198a013.
The synthesis and antihypertensive activity of a series of 2-benzamido-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]-quinolizines are reported. A number of these compounds exhibit extremely potent hypotensive properties (e.g., N-methylbenzamides 42, 48, and 50 and N-ethylbenzamide 53 cause drops of 110, 103, 79, and 83 mmHg, respectively, in systolic blood pressure in the spontaneous hypertensive rat at the screening dose of 50 mg/kg po). Structure-activity relationships for the entire series are discussed.
报道了一系列2-苯甲酰胺基-1,2,3,4,6,7,12,12b-八氢吲哚并[2,3-a]喹嗪的合成及其降压活性。其中许多化合物具有极强的降压特性（例如，在50mg/kg口服的筛选剂量下，N-甲基苯甲酰胺42、48和50以及N-乙基苯甲酰胺53可使自发性高血压大鼠的收缩压分别下降110、103、79和83mmHg）。讨论了整个系列的构效关系。
