The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6- alkyl CXCR2 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 15, 2014, Pages 3285-3290

  Porter, David W ^a   Bradley, Michelle ^a   Brown, Zarin ^a   Charlton, Steven J ^a   Cox, Brian ^a   Hunt, Peter ^a   Janus, Diana ^a   Lewis, Sarah ^a   Oakley, Paul ^a   O'Connor, Des ^a   Reilly, John ^a   Smith, Nichola ^a   Press, Neil J ^a  

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Chemokines; COPD; CXCR2; Neutrophils; Pyrimidine

Indexed keywords

2 [(2,3 DIFLUOROBENZYL)THIO] 6 [2 (HYDROXYMETHYL)CYCLOPROPYL) 5 ISOCYANOPYRIMIDIN 4 OL; CHEMOKINE RECEPTOR CXCR2 ANTAGONIST; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG; 2-((2,3-DIFLUOROBENZYL)THIO)-6-(2-(HYDROXYMETHYL)CYCLOPROPYL)-5-ISOCYANOPYRIMIDIN-4-OL; CHEMOKINE RECEPTOR CXCR2;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; DRUG SOLUBILITY; HUMAN; HUMAN CELL; IC 50; MICROSOME; MOLECULAR WEIGHT; NONHUMAN; PLASMA PROTEIN BINDING; RAT; REACTION OPTIMIZATION; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, INTERLEUKIN-8B; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84904055279     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.06.011     Document Type: Article

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