Studies on Agents with Vasodilator and .BETA.-Blocking Activities. II.
作者:Toshimi SEKI、Takayuki TAKEZAKI、Rikio OHUCHI、Hiroshi OHUYABU、Yoshitaka TANIMOTO、Takashi YAMAGUCHI、Norinobu SAITOH、Tsutomu ISHIMORI、Kikuo YASUDA
DOI:10.1248/cpb.43.247
日期:——
A series of phenoxypropanolamines having a hydrazinopyridazinyl moiety was synthesized. Their hypotensive and β-blocking activities were evaluated after intravenous administration of the compounds to anethetized rats.Some of them exhibited both activities. In particular, compound 20k is a candidate for clinical use due to its hypotensive activity, equal to that of hydralazine, and its β-blocking activity, 2.7-fold more potent than that of propranolol.
一系列含有哒嗪基肼结构的苯氧丙醇胺类化合物被合成,并通过静脉注射给麻醉大鼠后评估了它们的降压和β阻断活性。其中一些化合物显示了这两种活性。特别是化合物20k,由于其降压活性与肼达嗪相当,且β阻断活性比普萘洛尔强2.7倍,因此被认为是临床应用的候选药物。