Synthesis and bovine beta 3-adrenergic agonistic activities of a novel series of aryloxypropanolamines.
We synthesized a novel series of 21 aryloxypropanolamine compounds characterized by N-alkyl, aralkyl, and aryl substituents. The compounds showed potent beta 3-adrenergic agonistic activities in Chinese hamster ovary cells expressing the bovine beta 3-adrenoceptors with Kact and Ki values of 4.2 +/- 3.0 nM and 459 +/- 169 nM respectively, for the ligand with the best compromise between potency and affinity. Structure-activity relationships are discussed.
el Hadri
A
A
Département de Pharmacochimie Moléculaire, Université Joseph Fourier, France. Edwige.Nicolle@ujf-grenoble.fr
Nicolle
E
E
Guillaume
M C
MC
Leclerc
G
G
Pietri-Rouxel
F
F
Strosberg
A D
AD
Archimbault
P
P
D000262:Adenylyl Cyclases / Q000378:metabolism; D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D002478:Cells, Cultured; D004789:Enzyme Activation / Q000187:drug effects; D007202:Indicators and Reagents; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D007202:Indicators and Reagents; D011412:Propanolamines; D000262:Adenylyl Cyclases