Synthesis and Evaluation of Novel Phenylethanolamine Derivatives containing Acetanilides as Potent and Selective [beta]3-Adrenergic Receptor Agonists

In the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biologi...

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Published inChemical & pharmaceutical bulletin Vol. 58; no. 4; p. 533
Main Authors Maruyama, Tatsuya, Onda, Kenichi, Hayakawa, Masahiko, Suzuki, Takayuki, Kimizuka, Tetsuya, Matsui, Tetsuo, Takasu, Toshiyuki, Nagase, Itsuro, Hamada, Noritaka, Ohta, Mitsuaki
Format Journal Article
LanguageEnglish
Published Tokyo Japan Science and Technology Agency 01.04.2010
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Summary:In the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human β3-, β2-, and β1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5-methylthiazol-4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3-ylacetanilide (36h) derivatives showed potent agonistic activity at the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model.
ISSN:0009-2363
1347-5223