(Acylaryloxy)acetic acid diuretics. 1. (2-Alkyl- and 2,2-dialkyl-1-oxo-5-indanyloxy)acetic acids
| Autor: | Everett M. Schultz, Cragoe Edward J, Otto W. Woltersdorf, deSolms Sj |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Male
Uricosuric Double bond Pan troglodytes Substituent Administration Oral Natriuresis Acetates Medicinal chemistry Acetic acid chemistry.chemical_compound Structure-Activity Relationship Dogs Drug Discovery Molecule Animals Diuretics Alkyl chemistry.chemical_classification Bicyclic molecule Sodium Uricosuric Agents Carbonyl group Diuresis Rats chemistry Indans Injections Intravenous Molecular Medicine Female |
| Zdroj: | Journal of medicinal chemistry. 20(11) |
| ISSN: | 0022-2623 |
| Popis: | The discovery of the (acryloylaryloxy)acetic acids as a new class of potent diuretics prompted the investigation of related bicyclic compounds. Annelated analogues of the parent series, the (2-alkyl- and 2,2-dialkyl-1-oxo-5-indanyloxy)acetic acids, were the subjects of this study. Those compounds, unlike the monocyclic parent compound, lacked the double bond adjacent to the carbonyl group. More importantly, they possessed both saluretic and uricosuric properties. The optimal single 2-substituents for maximal saluretic and uricosuric activity were determined. In general, better activity was observed when a second 2-alkyl substituent (especially methyl) was present in the molecule. Replacement of the carboxy substituent by 5-tetrazolyl generally resulted in a reduction in activity. |
| Databáze: | OpenAIRE |
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