Synthesis and Evaluation of N-Phenyl-(2-aminothiazol-4-yl)acetamides with Phenoxypropanolamine Moiety as Selective β3-Adrenergic Receptor Agonists
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- Maruyama Tatsuya
- Drug Discovery Research, Astellas Pharma Inc.
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- Onda Kenichi
- Drug Discovery Research, Astellas Pharma Inc.
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- Suzuki Takayuki
- Drug Discovery Research, Astellas Pharma Inc.
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- Hayakawa Masahiko
- Drug Discovery Research, Astellas Pharma Inc.
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- Takahashi Takumi
- Drug Discovery Research, Astellas Pharma Inc.
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- Matsui Tetsuo
- Drug Discovery Research, Astellas Pharma Inc.
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- Takasu Toshiyuki
- Drug Discovery Research, Astellas Pharma Inc.
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- Nagase Itsuro
- Drug Discovery Research, Astellas Pharma Inc.
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- Ohta Mitsuaki
- Drug Discovery Research, Astellas Pharma Inc.
書誌事項
- タイトル別名
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- Synthesis and Evaluation of <i>N</i>-Phenyl-(2-aminothiazol-4-yl)acetamides with Phenoxypropanolamine Moiety as Selective β3-Adrenergic Receptor Agonists
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抄録
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.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 60 (5), 647-658, 2012
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679155814016
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- NII論文ID
- 130001852462
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- NII書誌ID
- AA00602100
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- COI
- 1:STN:280:DC%2BC38jgvFalsA%3D%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 023593504
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- PubMed
- 22689403
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可