Evaluation of a series of bicyclic CXCR2 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 2, 2008, Pages 798-803

  Walters, Iain ^a   Austin, Caroline ^a   Austin, Rupert ^a   Bonnert, Roger ^a   Cage, Peter ^a   Christie, Mark ^a   Ebden, Mark ^a   Gardiner, Stuart ^a   Grahames, Caroline ^a   Hill, Steven ^a   Hunt, Fraser ^a   Jewell, Robert ^a   Lewis, Shirley ^a   Martin, Iain ^a   Nicholls, David ^a   Robinson, David ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

CXCR2; Thiazolo 4,5 d pyrimidine 2(3H) one

Indexed keywords

2 AMINOTHIAZOLO[4,5 D]PYRIMIDINE; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR2; CHEMOKINE RECEPTOR CXCR2; PYRIMIDINE; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; NONHUMAN; PKA; RAT; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; DRUG EVALUATION, PRECLINICAL; PYRIMIDINES; RATS; RECEPTORS, INTERLEUKIN-8B; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 38349018273     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.039     Document Type: Article

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27. 50 values are means of at least two independent observations. Errors are within ±20%.
28. a's were determined from changes in UV spectra as a function of pH using a GLpKa auto titrator with DPAS attachment (Sirius Analytical Instruments Ltd, Forest Row, UK).
29. 2 values for antagonism determined.