Glamkowski E J, Reitano P A, Woodward D L
J Med Chem. 1977 Nov;20(11):1485-9. doi: 10.1021/jm00221a024.
A series of 3-(4-acylaminopiperazin-1-ylalkyl)indoles was synthesized and tested for antihypertensive activity. Compounds with no substituents in the indole portion of the molecule were generally most effective in lowering blood pressure in the spontaneous hypertensive rat model. Of these several analogues were very potent and lowered blood pressure more than 55 mmHg at oral doses of 100 mg/kg.
合成了一系列3-(4-酰基氨基哌嗪-1-基烷基)吲哚，并对其进行了抗高血压活性测试。在自发性高血压大鼠模型中，分子吲哚部分无取代基的化合物通常在降低血压方面最为有效。在这些类似物中，有几种非常有效，口服剂量为100mg/kg时可使血压降低超过55mmHg。
