Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 24, 2013, Pages 6890-6896

  Wilson, David M ^a   Apps, James ^a   Bailey, Nicholas ^a   Bamford, Mark J ^a   Beresford, Isabel J ^a   Brackenborough, Kim ^a   Briggs, Michael A ^a   Brough, Stephen ^a   Calver, Andrew R ^a   Crook, Barry ^a   Davis, Rebecca K ^a   Davis, Robert P ^a   Davis, Susannah ^a   Dean, David K ^a   Harris, Leanne ^a   Heslop, Teresa ^a   Holland, Vicky ^a   Jeffrey, Phillip ^a   Panchal, Terrance A ^a   Parr, Christopher A ^a   Quashie, Nigel ^a   Schogger, Joanne ^a   Sehmi, Sanjeet S ^a   Stean, Tania O ^a   Steadman, Jon G A ^a   Trail, Brenda ^a   Wald, Jeffrey ^a   Worby, Angela ^a   Takle, Andrew K ^a   Witherington, Jason ^a   Medhurst, Andrew D ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Clinical candidate; GPCR; H3 receptor; Histamine; Lead optimisation; Neurotransmitters; Receptor antagonists

Indexed keywords

6 (3 CYCLOBUTYL 2,3,4,5 TETRAHYDRO 1H 3 BENZAZEPIN 7 YLOXY) N METHYLNICOTINAMIDE; BENZAZEPINE DERIVATIVE; GSK 207040; GSK 239512; HISTAMINE H3 RECEPTOR ANTAGONIST; SCOPOLAMINE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ARTICLE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; HUMAN; NONHUMAN; PHYSICAL CHEMISTRY; RECOGNITION;

CLINICAL CANDIDATE; GPCR; H(3) RECEPTOR; HISTAMINE; LEAD OPTIMISATION; NEUROTRANSMITTERS; RECEPTOR ANTAGONISTS;

ANIMALS; BENZAZEPINES; DOGS; HALF-LIFE; HAPLORHINI; HISTAMINE H3 ANTAGONISTS; HUMANS; MALE; MICROSOMES, LIVER; NIACINAMIDE; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84888868762     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.09.090     Document Type: Article

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