Syntheses and .BETA.-adrenergic blocking activities of the optical isomers of 8-acetonyloxyl-5-(3-(3,4-dimethoxyphenethylamino)-2-hydroxypropoxy)-3,4-dihydrocarbostyril.
- 1 January 1981
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 29 (8) , 2157-2160
- https://doi.org/10.1248/cpb.29.2157
Abstract
The optical isomers of 8-acetonyloxy-5-[3-(3,4-dimethoxyphenethylamino)-2-hydroxypropoxy]-3,4-dihydrocarbostyril were prepared from the optically active epichlorhydrin, and their .beta.-adrenergic blocking activities were examined in guinea pigs. The (S)(-)-isomer was .apprx. 200 times more potent on atrial and 100 times more potent on tracheal preparations, and was also about 3 times more .beta.1-selective than the (R)(+)-isomer.This publication has 2 references indexed in Scilit:
- Syntheses and .BETA.-adrenergic blocking activities of carbostyril derivatives.CHEMICAL & PHARMACEUTICAL BULLETIN, 1981
- Synthesis of (R)- and (S)-epichlorohydrinThe Journal of Organic Chemistry, 1978