Synthesis and antihypertensive activity of 2-benzamido-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizines.
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.
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001549:Benzamides / Q000138:chemical synthesis / Q000494:pharmacology; D006973:Hypertension / Q000503:physiopathology; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology; D011807:Quinolizines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D001549:Benzamides; D007211:Indoles; D011807:Quinolizines