1034856-01-3Relevant academic research and scientific papers
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
Kallander, Lara S.,Washburn, David G.,Hoang, Tram H.,Frazee, James S.,Stoy, Patrick,Johnson, Latisha,Lu, Qing,Hammond, Marlys,Barton, Linda S.,Patterson, Jaclyn R.,Azzarano, Leonard M.,Nagilla, Rakesh,Madauss, Kevin P.,Williams, Shawn P.,Stewart, Eugene L.,Duraiswami, Chaya,Grygielko, Eugene T.,Xu, Xiaoping,Laping, Nicholas J.,Bray, Jeffrey D.,Thompson, Scott K.
scheme or table, p. 371 - 374 (2010/04/24)
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 in
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists
Thompson, Scott K.,Washburn, David G.,Frazee, James S.,Madauss, Kevin P.,Hoang, Tram H.,Lapinski, Leahann,Grygielko, Eugene T.,Glace, Lindsay E.,Trizna, Walter,Williams, Shawn P.,Duraiswami, Chaya,Bray, Jeffrey D.,Laping, Nicholas J.
experimental part, p. 4777 - 4780 (2010/06/11)
Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrrolidines
