The synthesis and SAR of novel diarylsulfone 11beta-HSD1 inhibitors.

Yan X; Wang Z; Sudom A; Cardozo M; DeGraffenreid M; Di Y; Fan P; He X; Jaen JC; Labelle M; Liu J; Ma J; McMinn D; Miao S; Sun D; Tang L; Tu H; Ursu S; Walker N; Ye Q; Powers JP

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The synthesis and SAR of novel diarylsulfone 11beta-HSD1 inhibitors.

机译：新型二芳基砜11β-HSD1抑制剂的合成和SAR。

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In this communication, human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11beta-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.

机译：在这种交流中，描述了一系列新的二芳基砜的人11beta-羟基类固醇脱氢酶1（11beta-HSD1）抑制活性。该系列产品的优化产生了几种具有出色药代动力学（PK）特性的高效11beta-HSD1抑制剂。化合物（S）-25在非人灵长类动物离体药效学模型中显示出优异的功效。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共5页
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Yan X; Wang Z; Sudom A; Cardozo M; DeGraffenreid M; Di Y; Fan P; He X; Jaen JC; Labelle M; Liu J; Ma J; McMinn D; Miao S; Sun D; Tang L; Tu H; Ursu S; Walker N; Ye Q; Powers JP;
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1. The synthesis and SAR of novel diarylsulfone 11beta-HSD1 inhibitors. [J] . Yan X, Wang Z, Sudom A, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

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The synthesis and SAR of novel diarylsulfone 11beta-HSD1 inhibitors.

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