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Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.

Abstract：

: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, α-substituent on the oxazolidinedione ring, central pyridinone core, and substituents on the central pyridinone core led to the discovery of potent EP(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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Morales-Ramos ÁI,Li YH,Hilfiker M,Mecom JS,Eidam P,Shi D,Tseng PS,Brooks C,Zhang D,Wang N,Jaworski JP,Morrow D,Fries H,Edwards R,Jin J

doi

10.1016/j.bmcl.2011.03.107

subject

Has Abstract

pub_date

2011-05-15 00:00:00

pages

2806-11

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00436-7

journal_volume

21

pub_type

杂志文章

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