New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent .beta.-adrenergic blocking properties
- 30 June 1985
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 28 (7) , 896-900
- https://doi.org/10.1021/jm00145a008
Abstract
The synthesis of R-(+) and S-(-) isomers of O-[3-(tert-butylamino)-2-hydroxypropyl] cyclopropyl methyl ketone oxime (falintolol [an antiglaucoma-drug]) is described. The syn and anti isomers of falintolol were obtained in 2 different ways from cyclopropyl methyl ketoxime or from falintolol. For comparison purposes, the enantiomers of the dicyclopropyl ketone oxime derivatives were also prepared. Structure-activity relationships are described. [B-Adrenergic activities were determined on the atria and trachea of guinea pigs.].This publication has 5 references indexed in Scilit:
- Synthesis and .beta.-adrenergic blocking activity of new aliphatic and alicyclic oxime ethersJournal of Medicinal Chemistry, 1984
- Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral .beta.-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluoreneJournal of Medicinal Chemistry, 1982
- Synthesis of (R)- and (S)-epichlorohydrinThe Journal of Organic Chemistry, 1978
- SOME QUANTITATIVE USES OF DRUG ANTAGONISTSBritish Journal of Pharmacology and Chemotherapy, 1959
- PDX, PAX AND PD'X VALUES IN THE ANALYSIS OF PHARMACODYNAMICS1957