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(Acylaryloxy)acetic acid diuretics. 1. (2-Alkyl- and 2,2-dialkyl-1-oxo-5-indanyloxy)acetic acids.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Woltersdorf OW Jr,deSolms SJ,Schultz EM,Cragoe EJ Jr

doi

10.1021/jm00221a010

subject

Has Abstract

pub_date

1977-11-01 00:00:00

pages

1400-8

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

20

pub_type

杂志文章

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