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-, 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.
Aubriot
Silvère
S
Département de Pharmacochimie Moléculaire, UMR-CNRS 5063, UFR de Pharmacie, Université Joseph Fourier, BP 138, F-38243 Meylan cedex, France.
Nicolle
Edwige
E
Lattier
Mireille
M
Morel
Cécile
C
Cao
Wenhong
W
Daniel
Kiefer W
KW
Collins
Sheila
S
Leclerc
Gérard
G
Faure
Patrice
P
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D019556:COS Cells; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D011412:Propanolamines / Q000737:chemistry / Q000494:pharmacology*
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D016166:Free Radical Scavengers; D011412:Propanolamines