Studies on agents with vasodilator and beta-blocking activities. I.
A series of hydrazinopyridazine derivatives combined with a beta-blocking side chain were synthesized. When they were given intravenously to anesthetized rats, some of them exhibited both hypotensive and beta-blocking activities. Their structure-activity relationships for hypotensive and beta-blocking activities are discussed. Compound 11c had the best profile and was selected for further study.
Research Division, Teikoku Hormone Manufacturing Co., Ltd., Kanagawa, Japan.
T
T
Seki
T
T
Takezaki
R
R
Ohuchi
H
H
Ohuyabu
T
T
Ishimori
K
K
Yasuda
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects*; D006339:Heart Rate / Q000187:drug effects*; D006835:Hydrazones / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007275:Injections, Intravenous; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D050198:Phenoxypropanolamines; D011724:Pyridazines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C090252:1-(2-(2-(3-isopropylidenehydrazino-6-pyridazinyloxy)ethyl)phenoxy)-3-isopropylamino-2-propanol; D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D006835:Hydrazones; D050198:Phenoxypropanolamines; D011724:Pyridazines; D014665:Vasodilator Agents