3,4-Diphenyl-1H-pyrazole-1-propanamine antidepressants
| Autor: | John E. Pearl, Allan G. Hlavac, Philip E. Hansen, Albert DeFelice, Martin E. Feigenson, Denis M. Bailey, Eugene R. Baizman |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
Male
Imipramine Serotonin Magnetic Resonance Spectroscopy Tertiary amine Stereochemistry Pyrazole Alkylation Motor Activity Medicinal chemistry chemistry.chemical_compound Mice Norepinephrine Drug Discovery medicine Animals Guanethidine Dose-Response Relationship Drug Chemistry Brain Biological activity Antidepressive Agents Rats Michael reaction Molecular Medicine Antidepressant Pyrazoles medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 28(2) |
| ISSN: | 0022-2623 |
| Popis: | A small series of compounds is described in which a narrow SAR has identified N,N-dimethyl-3,4-diphenyl-1H-pyrazole-1-propanamine, 3, as a potential antidepressant with reduced side effects. The isomeric N,N-dimethyl-4,5-diphenyl-1H-pyrazole-1-propanamine was completely inactive in the primary antidepressant screens. Compounds were synthesized by Michael addition of acrylonitrile to diphenylpyrazole followed by reductive alkylation of the resultant diphenylpyrazolepropionitriles. Compound 3 was equipotent with imipramine in standard antidepressant assays in animals but showed no significant anticholinergic action and did not antagonize the antihypertensive effects of clonidine and guanethidine. |
| Databáze: | OpenAIRE |
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