1256096-35-1Relevant articles and documents
Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective b 3-adrenergic receptor agonists
Maruyama, Tatsuya,Onda, Kenichi,Hayakawa, Masahiko,Suzuki, Takayuki,Kimizuka, Tetsuya,Matsui, Tetsuo,Takasu, Toshiyuki,Nagase, Itsuro,Hamada, Noritaka,Ohta, Mitsuaki
experimental part, p. 533 - 545 (2010/09/06)
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.