[A search for new beta-adrenoblockaders in the series of 5-phenoxymethyl-1,2,4-oxadiazole derivatives].
The experiments on anesthesized rats have revealed that some derivatives of (3-amino-2-hydroxypropoxy)phenomethyl-1,2,4-oxadiazole with the oxadiazole cycle at the o-position of the aromatic ring possess a significant beta-adrenoceptor blocking activity associated with alpha-adrenoceptor blocking properties. The most potent compound is 3-methyl-5-[2-(3-tret.butylamino-2-hydroxypropoxy) phenoxymethyl]-1,2,4-oxadiazole (Compound 1, prodolol) which is superior to propranolol, oxprenolol, and particularly labetalol in its beta-adrenoceptor blocking activity. The agent does not greatly differ from labetalol in its alpha-adrenoblocking activity. Proxodolol has been chosen for preclinical and clinical studies.
Mashkovskiĭ
M D
MD
Iuzhakov
S D
SD
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D002415:Cats; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009200:Myocardial Contraction / Q000187:drug effects; D010069:Oxadiazoles / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D010069:Oxadiazoles
Poisk novykh beta-adrenoblokatorov v riade proizvodnykh 5-fenoksimetil-1,2,4-oksadiazola.