Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen
| Autor: | Solomon S. Klioze, Victor J. Bauer, Harry M. Geyer |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Steric effects
Isobenzofuran Stereochemistry Heteroatom Tetrabenazine chemistry.chemical_element Nitrogen Antidepressive Agents chemistry.chemical_compound Mice Structure-Activity Relationship chemistry Piperidines Drug Discovery Methods Molecular Medicine Organic chemistry Animals Blepharoptosis Benzofurans |
| Zdroj: | Journal of medicinal chemistry. 20(4) |
| ISSN: | 0022-2623 |
| Popis: | The synthesis and antitetrabenazine activity of a series of N-heteroatom derivatives of 3-phenylspiro[isobenzofuran-1,4'-piperidines] are reported. Optimal antitetrabenazine activity is associated with compounds containing a sterically unhindered, basic nitrogen. Hydroxylamines 6, 11, 12, and 13 possess the most significant activity with ED50's of 1.4, 3.5, 4.7, and 4.0, respectively. |
| Databáze: | OpenAIRE |
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