Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 8, 2008, Pages 2684-2690

  Hall, Adrian ^a   Billinton, Andy ^a   Brown, Susan H ^a   Chowdhury, Anita ^a   Giblin, Gerard M P ^a   Goldsmith, Paul ^a   Hurst, David N ^a   Naylor, Alan ^a   Patel, Sadhana ^a   Scoccitti, Tiziana ^a   Theobald, Pamela J ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Conformational constraint; EP1 antagonist; Lead hopping; Pain; Scaffold hopping

Indexed keywords

ANALGESIC AGENT; CELECOXIB; EP 1 RECEPTOR ANTAGONIST; PROTEIN SERINE THREONINE KINASE INHIBITOR; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; HUMAN; HUMAN TISSUE; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; HUMANS; HYDROGEN BONDING; INDOLES; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS; RECEPTORS, PROSTAGLANDIN E; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 41849113120     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.03.018     Document Type: Article

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