Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists

Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 5; pp. 1200 - 1205
Main Authors HALL, Adrian, ATKINSON, Stephen, MICHEL, Anton D, NAYLOR, Alan, SWEETING, Jennifer A, BROWN, Susan H, CHESSELL, Iain P, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HEALY, Mark P, JANDU, Karamjit S, JOHNSON, Matthew R
Format Journal Article
LanguageEnglish
Published Oxford Elsevier 01.03.2007
Subjects
Biological and medical sciences
Humans
Inhibitory Concentration 50
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Protein Binding
Pyrroles - chemistry
Pyrroles - pharmacology
Receptors, Prostaglandin E - antagonists & inhibitors
Receptors, Prostaglandin E, EP1 Subtype
Structure-Activity Relationship
Sulfonamide
Organic chlorine compounds
In vitro
EP1 prostanoid receptor
Pyrrole derivatives
Biological fixation
Structure activity relation
Carboxylic acid replacement
Benzimidazole derivatives
Organic fluorine compounds
Pyrrole
Antagonist
EP1 antagonist
Chemical synthesis
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Summary:Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.12.021