Synthesis and Evaluation of N-Phenyl-(2-aminothiazol-4-yl)acetamides with Phenoxypropanolamine Moiety as 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 drugs for use in treating obesity and non-insulin dependent (type 2) diabetes, a series of N-phenyl-(2-aminothiazol-4-yl)acetamides with phenoxypropanolamine moiety were prepared and their biological activities against human β3-, β2-, and β1-ARs were evaluated. Among these compounds, N-phenyl-(2-phenylaminothiazol-4-yl)acetamide (4g), N-phenyl-(2-benzylaminothiazol-4-yl)acetamide (4j), and N-phenyl-[2-(3-methoxyphenyl)aminothiazol-4-yl]acetamide (6g) derivatives showed potent agonistic activity against the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent model of diabetes.

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.

• Matsui Tetsuo

  Drug Discovery Research, Astellas Pharma Inc.

• Takasu Toshiyuki

  Drug Discovery Research, Astellas Pharma Inc.

• Nagase Itsuro

  Drug Discovery Research, Astellas Pharma Inc.

• Ohta Mitsuaki

  Drug Discovery Research, Astellas Pharma Inc.

• Hayakawa Masahiko

  Drug Discovery Res. Astellas Pharma Inc.

• Takahashi Takumi

  Drug Discovery Research, Astellas Pharma Inc.

関連論文

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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
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• Antidiabetic Effects of SGLT2-Selective Inhibitor Ipragliflozin in Streptozotocin-Nicotinamide-Induced Mildly Diabetic Mice

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