کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372496 | 981870 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Improving the developability profile of pyrrolidine progesterone receptor partial agonists Improving the developability profile of pyrrolidine progesterone receptor partial agonists](/preview/png/1372496.png)
چکیده انگلیسی
The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The basic pyrrolidine amine was intentionally converted to a sulfonamide, carbamate, or amide to address these liabilities. The evaluation of the degree of partial agonism for these non-basic pyrrolidine derivatives and demonstration of their efficacy in an in vivo model of endometriosis is disclosed herein.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 1, 1 January 2010, Pages 371–374
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 1, 1 January 2010, Pages 371–374
نویسندگان
Lara S. Kallander, David G. Washburn, Tram H. Hoang, James S. Frazee, Patrick Stoy, Latisha Johnson, Qing Lu, Marlys Hammond, Linda S. Barton, Jaclyn R. Patterson, Leonard M. Azzarano, Rakesh Nagilla, Kevin P. Madauss, Shawn P. Williams,