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Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 1, 2014, Pages 72-76

The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists

(16) Porter, David W a Bradley, Michelle a Brown, Zarin a Canova, Riccardo b Charlton, Steven a Cox, Brian a Hunt, Peter a Kolarik, David b Lewis, Sarah a O'Connor, Des a Reilly, John a Spanka, Carsten b Tedaldi, Lauren a Watson, Simon J a Wermuth, Roland b Press, Neil J a

a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH (United States)

b NOVARTIS PHARMA AG (Switzerland)

Author keywords

Chemokines; COPD; CXCR2; Neutrophils; Pyrazolopyrimidine; Triazolopyrimidine

Indexed keywords

2 BENZYL 5 (((2,3 DIFLUOROPHENYL)THIO)METHYL) [1,2,4]TRIAZOLO[1,5 ALPHA]PYRIMIDIN 7 OL; 2 METHYL 5 ((PHENYLTHIO)METHYL)PYRAZOLO[1,5 ALPHA]PYRIMIDIN 7 OL; ALKYL GROUP; AZD 5069; CHEMOKINE RECEPTOR CXCR2 ANTAGONIST; DANIRIXIN; NAVARIXIN; PYRIMIDINE DERIVATIVE; THIOL DERIVATIVE; UNCLASSIFIED DRUG; 2 BENZYL 5 [[(2,3 DIFLUOROPHENYL)THIO]METHYL] [1,2,4]TRIAZOLO[1,5 A]PYRIMIDIN 7 OL; PYRAZOLE DERIVATIVE; PYRAZOLOPYRIMIDINE 2 METHYL 5 [(PHENYLTHIO)METHYL]PYRAZOLO[1,5 A]PYRIMIDIN 7 OL; TRIAZOLOPYRIMIDINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CLINICAL TRIAL (TOPIC); DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG SCREENING; HALOGENATION; HIGH TEMPERATURE; HUMAN; HUMAN CELL; LIPOPHILICITY; MICROSOME; NONHUMAN; PLASMA PROTEIN BINDING; RAT; BINDING AFFINITY; GLUCURONIDATION; IC50; MOLECULAR WEIGHT; STRUCTURE ACTIVITY RELATION;

CHEMOKINES; COPD; CXCR2; NEUTROPHILS; PYRAZOLOPYRIMIDINE; TRIAZOLOPYRIMIDINE;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MOLECULAR STRUCTURE; PYRAZOLES; PYRIMIDINES; RECEPTORS, CCR2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84891482449 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2013.11.074 Document Type: Article

Times cited : (22)

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