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Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.

Abstract：

:A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Optimization of the substitution patterns on the three aromatic rings led to the identification of high affinity EP1 receptor antagonists. The derivative with highest affinity displayed a binding IC50 of 2.5 nM (pIC50 8.6).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hall A,Brown SH,Chowdhury A,Giblin GM,Gibson M,Healy MP,Livermore DG,Wilson RJ,Naylor A,Rawlings DA,Roman S,Ward E,Willay C

doi

10.1016/j.bmcl.2007.06.014

subject

Has Abstract

pub_date

2007-08-15 00:00:00

pages

4450-5

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00694-4

journal_volume

17

pub_type

杂志文章

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