Synthesis and pharmacological evaluation of 7-substituted procaterol derivatives.
A series of procaterol derivatives having a substituent at the 7-position of the carbostyril moiety was synthesized. Halogenation of procaterol and its homologues gave the 7-halogeno derivatives (3). Nitration of the procaterol analogues afforded the 7-nitro derivatives (4), and the catalytic reduction of 4 gave the 7-amino derivatives (5). These compounds showed weak beta-adrenoceptor stimulant activities in anesthetized dog.
Yoshizaki
S
S
Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Japan.
Tamada
S
S
Yo
E
E
Umezato
M
M
D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D016084:Bronchoconstriction / Q000187:drug effects; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D017265:Procaterol / Q000031:analogs & derivatives* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000318:Adrenergic beta-Agonists; D017265:Procaterol