Literature DB >> 17574410

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

Adrian Hall1, Susan H Brown, Anita Chowdhury, Gerard M P Giblin, Mairi Gibson, Mark P Healy, David G Livermore, Richard J McArthur Wilson, Alan Naylor, D Anthony Rawlings, Shilina Roman, Emma Ward, Caroline Willay.   

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).

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Year:  2007        PMID: 17574410     DOI: 10.1016/j.bmcl.2007.06.014

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  A new and efficient method for the synthesis of novel 3-acetyl coumarins oxadiazoles derivatives with expected biological activity.

Authors:  Abdullah Sulaiman Al-Ayed; Naceur Hamdi
Journal:  Molecules       Date:  2014-01-14       Impact factor: 4.411

2.  Syntheses of diheterocyclic compounds based on 2-thioacetohydrazide-5,7-dimethyl-1,2,4-triazolo[1,5-a]- pyrimidine.

Authors:  Zu-Ming Liu; Qiong Chen; Chao-Nan Chen; Hai-Yang Tu; Guang-Fu Yang
Journal:  Molecules       Date:  2008-06-13       Impact factor: 4.411

  2 in total

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