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

Autor:	Rakesh Nagilla, Sharada Manns, Eugene L. Stewart, Marlys Hammond, Tram H. Hoang, Scott K. Thompson, Walter Trizna, Chaya Duraiswami, Eugene T. Grygielko, Thuy B. Tran, James S. Frazee, Kevin P. Madauss, Johnson Latisha C, Shawn P. Williams, Lindsay E. Glace, David G. Washburn, Jeffrey D. Bray
Rok vydání:	2009
Předmět:	Agonist medicine.drug_class Stereochemistry Clinical Biochemistry hERG Administration Oral Pharmaceutical Science Pharmacology Biochemistry Partial agonist Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Progesterone receptor medicine Animals Humans Pyrrolidinones Molecular Biology Binding Sites biology Organic Chemistry Haplorhini Ether-A-Go-Go Potassium Channels Rats Nuclear receptor chemistry biology.protein Molecular Medicine Receptors Progesterone Lead compound
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:4664-4668
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e117925c53a26178fac52da1fa94885 https://doi.org/10.1016/j.bmcl.2009.06.081 Zobrazit plný text záznamu Full Text from ScienceDirect