Referenced in: none

Automatically associated channels: Kv11.1

Title: Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.

Authors: David G Washburn, Tram H Hoang, James S Frazee, Latisha Johnson, Marlys Hammond, Sharada Manns, Kevin P Madauss, Shawn P Williams, Chaya Duraiswami, Thuy B Tran, Eugene L Stewart, Eugene T Grygielko, Lindsay E Glace, Walter Trizna, Rakesh Nagilla, Jeffrey D Bray, Scott K Thompson

Journal, date & volume: Bioorg. Med. Chem. Lett., 2009 Aug 15 , 19, 4664-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/19616429

Abstract
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In addition, these compounds had improved selectivity against hERG channel inhibition.