Nomoto Y, Takai H, Hirata T, Teranishi M, Ohno T, Kubo K
Tokyo Research Laboratory, Kyowa Hakko Kogyo Co., Ltd., Japan.
Chem Pharm Bull (Tokyo). 1990 Nov;38(11):3014-9. doi: 10.1248/cpb.38.3014.
A series of novel 1-(6,7-dimethoxy-4-quinazolinyl)piperidines carrying substituted hydantoin and 2-thiohydantoin rings was synthesized and examined for cardiotonic activity in anesthetized dogs. Introduction of isopropyl and sec-butyl group at the 5-position of the hydantoin and thiohydantoin rings led to potent inotropic activity. Effects of insertion of an alkyl chain between the piperidine and the hydantoin rings were also examined. The structural requirements necessary for optimal cardiotonic activity within the series were investigated.
合成了一系列带有取代乙内酰脲和2-硫代乙内酰脲环的新型1-(6,7-二甲氧基-4-喹唑啉基)哌啶，并在麻醉犬中检测其强心活性。在乙内酰脲和硫代乙内酰脲环的5-位引入异丙基和仲丁基导致了强效的正性肌力活性。还研究了在哌啶和乙内酰脲环之间插入烷基链的影响。研究了该系列中实现最佳强心活性所需的结构要求。
