کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362558 | 981490 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.
The synthesis and SAR of a series of diarylsulfone inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a non-human primate ex vivo enzyme inhibition model.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7071–7075
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7071–7075
نویسندگان
Xuelei Yan, Zhulun Wang, Athena Sudom, Mario Cardozo, Michael DeGraffenreid, Yongmei Di, Pingchen Fan, Xiao He, Juan C. Jaen, Marc Labelle, Jinsong Liu, Ji Ma, Dustin McMinn, Shichang Miao, Daqing Sun, Liang Tang, Hua Tu, Stefania Ursu, Nigel Walker,