New bicyclic antidepressant agent. Synthesis and activity of napactadine and related compounds
| Autor: | Philip J. Shea, Randy Eyster, Abdul H. Abdallah, James R. McCarthy, Albert J. Schuster, Donald L. Wright |
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| Rok vydání: | 1985 |
| Předmět: |
Male
Reserpine Chemical Phenomena Stereochemistry Hydrochloride Amidines Imipramine Amidine chemistry.chemical_compound Mice Norepinephrine Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Animals Blepharoptosis NAPACTADINE Cerebral Cortex Bicyclic molecule Chemistry Depression Yohimbine Biological activity Drug Synergism Electric Stimulation Rats Aggression Molecular Medicine Antidepressant Drug Evaluation medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 28(11) |
| ISSN: | 0022-2623 |
| Popis: | A number of N,N'-dialkylarylamidines were synthesized and evaluated for antidepressant activity. Several of these compounds were synthesized from the corresponding nitriles by a new method. Slight structural modification in the series caused a marked change in biological activity and led to compounds as active as imipramine. The arylacetamidine, N,N'-dimethyl-2-naphthaleneethanimidamide hydrochloride (33) (napactadine) was selected for clinical study. Forty-eight additional analogues of 33, including a number of N-alkylamidines, were prepared. |
| Databáze: | OpenAIRE |
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