beta-Adrenergic blocking agents with acute antihypertensive activity
| Autor: | Ralph Hirschmann, R. Hall, George F. Lundell, Charles S. Sweet, Gerald S. Ponticello, John J. Baldwin, Edward L. Engelhardt, Ludden Ct, A. Scriabine, N. N. Share |
|---|---|
| Rok vydání: | 1979 |
| Předmět: |
Male
Stereochemistry Adrenergic beta-Antagonists Blood Pressure Ring (chemistry) Iliac Artery chemistry.chemical_compound Structure-Activity Relationship Dogs Heart Rate Drug Discovery Imidazole Animals Beta (finance) Alkyl Antihypertensive Agents chemistry.chemical_classification Trifluoromethyl Beta-adrenergic blocking agent Blocking (radio) Aryl Airway Resistance Imidazoles Heart Rats chemistry Organ Specificity Regional Blood Flow Hypertension Molecular Medicine Female |
| Zdroj: | Journal of medicinal chemistry. 22(6) |
| ISSN: | 0022-2623 |
| Popis: | Modification of the pharmacological profile of the vasodilating/beta-adrenergic blocking agent 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-4-(trifluoromethyl)imidazole (1) has been investigated. Introduction of selected substitutents onto the imidazole ring, in place of the trifluoromethyl group, has yielded highly cardioselective beta-adrenergic blocking agents such as 7, 17, and 18. The placement of alkyl or chloro groups onto the aryl ring of 1, as illustrated by 33, has produced a class of compounds characterized as antihypertensive beta-adrenergic blocking agents. In these examples, the acute antihypertensive activity does not appear to be due to either vasodilating or beta 2-agonist properties. |
| Databáze: | OpenAIRE |
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