کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588784 | 981505 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors](/preview/png/10588784.png)
چکیده انگلیسی
A series of carboxylic acid glycogen phosphorylase inhibitors, which have potential as oral antidiabetic agents, is described. Defining and applying simple physicochemical design criteria was used to assess the opportunity and to focus synthetic efforts on compounds with the greatest probability of success. The study led to compound 17, which exhibits a good balance of properties including potent inhibition of recombinant human liver glycogen phosphorylase in vitro, a good DMPK profile including excellent bioavailability and low clearance and good in vivo activity in a glucagon challenge model of diabetes in Zucker rats.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 12, 15 June 2010, Pages 3511-3514
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 12, 15 June 2010, Pages 3511-3514
نویسندگان
Stuart N.L. Bennett, Andrew D. Campbell, Andrew Hancock, Craig Johnstone, Peter W. Kenny, Adrian Pickup, Alleyn T. Plowright, Nidhal Selmi, Iain Simpson, Andy Stocker, David P. Whalley, Paul R.O. Whittamore,