New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties

A series of 13 novel hybrid molecules designed to possess both free radical scavenging activity and to stimulate the beta(3)-adrenoceptors in order to improve antidiabetic effect and to restore insulin sensitivity was synthesized and evaluated. Compounds were of quinolyl-, isoquinolyl-, pyridoindoly...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-01, Vol.12 (2), p.209-212
Main Authors: Aubriot, Silvère, Nicolle, Edwige, Lattier, Mireille, Morel, Cécile, Cao, Wenhong, Daniel, Kiefer W, Collins, Sheila, Leclerc, Gérard, Faure, Patrice
Format: Article
Language:English
Subjects:
Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Agonists - chemistry
Adrenergic beta-Agonists - pharmacology
Animals
COS Cells
Free Radical Scavengers - chemistry
Free Radical Scavengers - pharmacology
Humans
Propanolamines - chemistry
Propanolamines - pharmacology
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Summary:A series of 13 novel hybrid molecules designed to possess both free radical scavenging activity and to stimulate the beta(3)-adrenoceptors in order to improve antidiabetic effect and to restore insulin sensitivity was synthesized and evaluated. Compounds were of quinolyl-, isoquinolyl-, pyridoindolyl- or carbazolyloxypropanolamine structure with a terminal amino group of benzopyranolyl-, di-tert-butylphenolyl- or methoxyindolyl-type. Some of the products possessed both the expected activities.
ISSN:0960-894X
DOI:10.1016/S0960-894X(01)00716-8