Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP sub(3 receptor antagonists)

Multiple regions of the 3-oxazolidinedione-6-naphthyl-pyridinone series identified via high throughput screening were explored. SAR studies of these regions including the left-hand side oxazolidinedione moiety, alpha -substituent on the oxazolidinedione ring, central pyridinone core, and substituent...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 21; no. 10; pp. 2806 - 2811
Main Authors Morales-Ramos, Angel I, Li, Yue H, Hilfiker, Mark, Mecom, John S, Eidam, Patrick, Shi, Dongchuan, Tseng, Pei-San, Brooks, Carl, Zhang, David, Wang, Ning, Jaworski, Jon-Paul, Morrow, Dwight, Fries, Harvey, Edwards, Richard, Jin, Jian
Format Journal Article
LanguageEnglish
Published 15.05.2011
Online AccessGet full text

Cover

More Information
Summary:Multiple regions of the 3-oxazolidinedione-6-naphthyl-pyridinone series identified via high throughput screening were explored. SAR studies of these regions including the left-hand side oxazolidinedione moiety, alpha -substituent on the oxazolidinedione ring, central pyridinone core, and substituents on the central pyridinone core led to the discovery of potent EP sub(3 receptor antagonists such as compound 29 which possesses outstanding rat pharmacokinetic properties. Synthesis and SAR of these novel compounds and DMPK properties of representative compounds are discussed.)
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2011.03.107