Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists.
Bioorg Med Chem Lett
; 25(7): 1616-20, 2015 Apr 01.
Article
en En
| MEDLINE
| ID: mdl-25708618
ABSTRACT
Antagonism of the chemokine receptor CXCR2 has been proposed as a strategy for the treatment of inflammatory diseases such as arthritis, chronic obstructive pulmonary disease and asthma. Earlier series of bicyclic CXCR2 antagonists discovered at AstraZeneca were shown to have low solubility and poor oral bioavailability. In this Letter we describe the design, synthesis and characterisation of a new series of monocyclic CXCR2 antagonists with improved solubility and good pharmacokinetic profiles.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Receptores de Interleucina-8B
/
Descubrimiento de Drogas
/
Amidas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2015
Tipo del documento:
Article
País de afiliación:
Reino Unido