Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.

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Cerelli MJ, Curtis DL, Dunn JP, Nelson PH, Peak TM, Waterbury LD

Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.

J Med Chem. 1986 Nov;29(11):2347-51.

PubMed ID
3097317 [ View in PubMed
]
Abstract

A number of dibenztropone, dibenzsuberone, dibenzoxepin, and dibenzthiepin acetic acids were synthesized and tested for antiinflammatory/analgesic activity and also for their ability to inhibit rabbit lens aldose reductase (AR). It was found that the structural requirements for antiinflammatory/analgesic activity, believed to be mediated by inhibition of cyclooxygenase, were much more stringent than were those for AR inhibition. For example, the introduction of a hydroxyl group into positions 1, 4, 6, 7, or 8 on dibenzsuberone-2-acetic acid (1a) had relatively little effect on AR inhibition, but caused wide variations in antiinflammatory/analgesic activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SorbinilAldose reductaseIC 50 (nM)67N/AN/ADetails