Synthesis and Evaluation of Novel Phenylethanolamine Derivatives containing Acetanilides as Potent and Selective β3-Adrenergic Receptor Agonists

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概要

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• 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.

著者

• Maruyama Tatsuya

  Drug Discovery Research, Astellas Pharma Inc.

• Onda Kenichi

  Drug Discovery Research, Astellas Pharma Inc.

• Hayakawa Masahiko

  Drug Discovery Research, Astellas Pharma Inc.

• Suzuki Takayuki

  Drug Discovery Research, Astellas Pharma Inc.

• Kimizuka Tetsuya

  Drug Discovery Research, Astellas Pharma Inc.

• Matsui Tetsuo

  Drug Discovery Research, Astellas Pharma Inc.

• Takasu Toshiyuki

  Drug Discovery Research, Astellas Pharma Inc.

• Nagase Itsuro

  Drug Discovery Research, Astellas Pharma Inc.

• Hamada Noritaka

  Drug Discovery Research, Astellas Pharma Inc.

• Ohta Mitsuaki

  Drug Discovery Research, Astellas Pharma Inc.

• Hayakawa Masahiko

  Drug Discovery Res. Astellas Pharma Inc.

関連論文

• Synthesis and Evaluation of Novel Phenylethanolamine Derivatives containing Acetanilides as Potent and Selective β3-Adrenergic Receptor Agonists
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• Synthesis and Evaluation of N-Phenyl-(2-aminothiazol-4-yl)acetamides with Phenoxypropanolamine Moiety as Selective β3-Adrenergic Receptor Agonists
• Antidiabetic Effects of SGLT2-Selective Inhibitor Ipragliflozin in Streptozotocin–Nicotinamide-Induced Mildly Diabetic Mice
• Synthesis and Pharmacological Evaluation of 2-(1-Alkylpiperidin-4-yl)-N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]acetamide Derivatives as Novel Antihypertensive Agents
• Antidiabetic Effects of SGLT2-Selective Inhibitor Ipragliflozin in Streptozotocin-Nicotinamide-Induced Mildly Diabetic Mice

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