Synthesis and bovine β3-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 β3-adrenergic agonistic activities in Chinese hamster ovary cells expressing the bovine β3-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,Nicolle,Guillaume,Leclerc,Pietri-Rouxel,Strosberg,Archimbault
p. 517 - 522
(2007/10/03)
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