Yoshizaki S, Manabe Y, Tamada S, Nakagawa K, Tei S
J Med Chem. 1977 Aug;20(8):1103-4. doi: 10.1021/jm00218a024.
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.
新型强效β2-选择性支气管扩张剂赤式-5-(1-羟基-2-异丙氨基丁基)-8-羟基喹啉酮(1)的异构体，通过化合物1的光学拆分以及赤式异构体向苏式异构体的转化得以合成。对这些异构体进行了抑制组胺诱导的支气管痉挛以及提高麻醉犬心率活性的测试。外消旋体和(-)-赤式-1显示出强效β2-选择性支气管扩张活性。在这些异构体中，(-)-赤式-1活性最高，(+)-赤式-1活性最低。
