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