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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
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
نویسندگان
, , , , , , , , , , , , , , , , , , ,