Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers.

Article Details

Citation

Leclerc G, Bieth N, Schwartz J

Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers.

J Med Chem. 1980 Jun;23(6):620-4.

PubMed ID
6104730 [ View in PubMed
]
Abstract

New beta-adrenergic blocking agents, most of which do not contain an aromatic nucleus, were synthesized. They were derived either from alkylamino-aliphatic oxime ethers or alkylamino-aliphatic ethers. Most active among these are O-[3-(tert-butylamino)-2-hydroxypropyl]acetoxime (8; trachea pA2 = 7.65) and 1-isobutoxy-3-(tert-butylamino)-2-propanol (15; trachea pA2 = 7.49), both of which displayed bronchoselectivity (beta 2/beta 1 ratio approximately 15). The role and importance of the aromatic nucleus in this class of compounds are discussed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PropranololBeta-1 adrenergic receptorKd (nM)2.4N/AN/ADetails