2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents
| Autor: | Peter A. Easson, Bui Vinh Lap Bui Vinh Lap, Diana M. Temple, Gordon L. Letts, Chen H. Lim, Lyall R. Williams |
|---|---|
| Rok vydání: | 1978 |
| Předmět: |
Beta-adrenergic blocking agent
Chemistry Stereochemistry Adrenergic beta-Antagonists Guinea Pigs Substituent Antagonist Isoproterenol Ethanolamines Heart In Vitro Techniques Trachea chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Molecular Medicine Structure–activity relationship Potency Animals Selectivity |
| Zdroj: | Journal of medicinal chemistry. 21(10) |
| ISSN: | 0022-2623 |
| Popis: | The effect of the introduction of a 2-methoxy substituent on the beta-adrenergic antagonistic properties of a series of 3- and 4-substituted phenylethanolamines (1) was studied. Both the series of bromo- and methyl-substituted compounds behaved similarly, indicating that electronic forces are not significant in determining beta-adrenergic antagonist activity. When compared with the corresponding phenylethanolamines without a 2-methoxy substitutent, the 2-methoxy-4-substituted derivatives (3a and 3d) had enhanced potency and selectivity but the 2,3- (3b and 3e) and the 2,5-disubstitution patterns (3c and 3f) showed a loss of activity. The inconsistent changes in activity prevented any firm conclusions being made about the effect of the ether oxygen and the beta-adrenoceptor antagonistic activity of phenoxypropanolamines. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|