Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H 1 antagonists. Part II: Optimising in vivo clearance

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 24, 2012, Pages 7707-7710

  Furber, Mark ^b   Alcaraz, Lilian ^a   Luckhurst, Christopher ^a   Bahl, Ash ^a   Beaton, Haydn ^a   Bowers, Keith ^a   Collington, John ^a   Denton, Rebecca ^a   Donald, David ^a   Kinchin, Elizabeth ^a   MacDonald, Cathy ^a   Rigby, Aaron ^a   Riley, Rob ^a   Soars, Matt ^a   Springthorpe, Brian ^a   Webborn, Peter ^a  

^a ASTRAZENECA   (United Kingdom)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

Allergic disease; CCR3; Chemokine antagonist; Dual inhibitor; H1; Receptor antagonist

Indexed keywords

CHEMOKINE RECEPTOR ANTAGONIST; PHENOXYPIPERIDINE HYDROXYAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DECARBOXYLATION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DEVELOPMENT; DRUG DISTRIBUTION; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYDROLYSIS; IC 50; IN VITRO STUDY; IN VIVO STUDY; LIVER BLOOD FLOW; NONHUMAN; PHARMACOKINETICS; RAT; REACTION TIME;

ANIMALS; DOGS; DRUG DISCOVERY; HEPATOCYTES; HUMANS; MICROSOMES, LIVER; PIPERIDINES; RATS; RECEPTORS, CCR3; RECEPTORS, HISTAMINE H1; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION;

EID: 84870238399     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.09.112     Document Type: Article

References (1)

1. C.A. Luckhurst, M. Furber, L. Alcaraz, A. Bahl, H. Beaton, K. Bowers, J. Collington, R. Denton, D. Donald, E. Kinchin, C. MacDonald, A. Rigby, R. Riley, M. Soars, B. Springthorpe, and P. Webborn Bioorg. Med. Chem. Lett. 2012 http://dx.doi.org/10.1016/j.bmcl.2012.09.113