Isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril, a new bronchodilator.
The isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril (1), a new potent and beta2-selective bronchodilator, were synthesized by optical resolution of compound 1 and inversion of the erythro to the threo isomers. The isomers were tested for activities to inhibit histamine-induced bronchospasm and to increase the heart rate of anesthetized dogs. Racemic and (-)-erythro-1 showed potent and beta2-selective bronchodilater activities. Among the isomers, (-)-erythro-1 showed the highest activities and (+)-erythro-1 showed the lowest.
D000818:Animals; D001986:Bronchial Spasm / Q000139:chemically induced / Q000503:physiopathology; D001993:Bronchodilator Agents / Q000138:chemical synthesis*; D004285:Dogs; D006339:Heart Rate / Q000187:drug effects; D006632:Histamine / Q000494:pharmacology; D006912:Hydroxyquinolines / Q000138:chemical synthesis*; D007536:Isomerism; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male
D001993:Bronchodilator Agents; D006912:Hydroxyquinolines; D006632:Histamine; D007545:Isoproterenol