(Acylaryloxy)acetic acid diuretics. 2. (2-Alkyl-2-aryl-1-oxo-5-indanyloxy)acetic acids
| Autor: | Otto W. Woltersdorf, L. Sherman Watson, G. M. Fanelli, Edward J. Cragoe, Desolms S Jane |
|---|---|
| Rok vydání: | 1978 |
| Předmět: |
Uricosuric
Pan troglodytes Natriuresis Acetates Alkylation Medicinal chemistry Structure-Activity Relationship chemistry.chemical_compound Acetic acid Dogs Chlorides Drug Discovery Animals Phenols Diuretics Alkyl chemistry.chemical_classification Indacrinone Aryl Stereoisomerism Uricosuric Agents Diuretic Activity Rats chemistry Potassium Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 21:437-443 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00203a006 |
| Popis: | The introduction of an aryl group at the 2 position of the uricosuric diuretics, (1-oxo-2-alkyl-5-indanyloxy)acetic acids, provided compounds with markedly increased potency over their monosubstituted precursors. These compounds were synthesized either by arylation of the corresponding 2-alkyl-5-methoxy-1-indanones with diaryliodonium salts or by alkylation of the 2-aryl-5-methoxy-1-indanones which were cleaved to the corresponding phenols and then converted to the desired oxyacetic acids. Systematic structural variation of the 2-arylindanyloxyacetic acids provided aryl-substituted compounds with varying degrees of uricosuric and diuretic activity. |
| Databáze: | OpenAIRE |
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