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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
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.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 1, 1 January 2010, Pages 371–374
نویسندگان
, , , , , , , , , , , , , ,