The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 12, 2012, Pages 3895-3899

  Cumming, John G ^a   Bower, Justin F ^a,b   Waterson, David ^a,c   Faull, Alan ^a   Poyser, Philip J ^a   Turner, Paul ^a   McDermott, Benjamin ^a   Campbell, Andrew D ^a   Hudson, Julian ^a   James, Michael ^a   Winter, Jon ^a   Wood, Christine ^a  

^a ASTRAZENECA   (United Kingdom)

^b BEATSON INSTITUTE FOR CANCER RESEARCH   (United Kingdom)

^c Medicines for Malaria Venture   (Switzerland)

Author keywords

CCR2 antagonists; Chemokine receptor; hERG

Indexed keywords

CHEMOKINE RECEPTOR CCR2; CHEMOKINE RECEPTOR CCR2 ANTAGONIST; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; G PROTEIN COUPLED RECEPTOR; MONOCYTE CHEMOTACTIC PROTEIN 1; N (3,4 DICHLOROPHENYL) 4 [(2R) 4 ISOPROPYLPIPERAZINE 2 CARBONYL]PIPERAZINE 1 CARBOXAMIDE; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ARTICLE; CALCIUM TRANSPORT; CELL MEMBRANE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG SYNTHESIS; HUMAN; LIPOPHILICITY; NONHUMAN; PROTEIN BINDING; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTI-INFLAMMATORY AGENTS; CALCIUM; DOGS; DRUG DESIGN; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; HYDROPHOBIC AND HYDROPHILIC INTERACTIONS; INFLAMMATION; PIPERAZINES; PROTEIN BINDING; RATS; RECEPTORS, CCR2;

EID: 84861575210     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.04.118     Document Type: Article

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