New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties.
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Bouzoubaa M, Leclerc G, Rakhit S, Andermann G
New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties.
J Med Chem. 1985 Jul;28(7):896-900.
- PubMed ID
- 2861288 [ View in PubMed]
- Abstract
The synthesis of R-(+) and S-(-) isomers of O-[3-tert-butylamino)-2-hydroxypropyl] cyclopropyl methyl ketone oxime (falintolol) is described. The syn and anti isomers of falintolol were obtained in two 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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Propranolol Beta-1 adrenergic receptor Kd (nM) 2.4 N/A N/A Details