Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 14, 2008, Pages 4027-4032

  Hall, Adrian ^a   Billinton, Andy ^a   Bristow, Alan K ^b   Brown, Susan H ^a   Chowdhury, Anita ^a   Cutler, Leanne ^a   Giblin, Gerard M P ^a   Goldsmith, Paul ^a   Hayhow, Thomas G ^a   Kilford, Ian R ^a   Naylor, Alan ^a   Passingham, Barry ^a   Rawlings, D Anthony ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Pharmaceutical Development   (United Kingdom)

Author keywords

Amide EP1 antagonist; Brain penetration; CNS penetration; Improved solubility; Non acidic EP1 antagonist; Oral absorption; Oral exposure; Solubility

Indexed keywords

AMIDE; CARBOXYLIC ACID; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; PYRAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; DISTRIBUTION VOLUME; DRUG ABSORPTION; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; IC 50; NONHUMAN; PHARMACOPHORE; RAT; STRUCTURE ACTIVITY RELATION;

AMIDES; BRAIN; CARBOXYLIC ACIDS; CENTRAL NERVOUS SYSTEM; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; ISOQUINOLINES; MODELS, CHEMICAL; MOLECULAR STRUCTURE; PYRAZOLES; RECEPTORS, PROSTAGLANDIN E; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 47149102125     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.118     Document Type: Article

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