Seki T, Nakao T, Masuda T, Hasumi K, Gotanda K, Ishimori T, Honma S, Minami N, Shibata K, Yasuda K
Research Division, Teikoku Manufacturing Co., Ltd., Kanagawa, Japan.
Chem Pharm Bull (Tokyo). 1996 Nov;44(11):2061-9. doi: 10.1248/cpb.44.2061.
A series of novel pyridazinone derivatives (II) having a phenoxypropanolamine moiety was synthesized. Their hypotensive and beta-blocking activities were evaluated after intravenous administration of the compounds to anesthetized rats. Among them, the 5-chloro-2-cyanophenoxy derivative (29) showed the promising dual activities and was selected for further studies.
合成了一系列具有苯氧丙醇胺部分的新型哒嗪酮衍生物(II)。将这些化合物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,5-氯-2-氰基苯氧基衍生物(29)表现出有前景的双重活性,并被选作进一步研究。