Evaluation of a series of bicyclic CXCR2 antagonists.

Abstract:

:The CXCR2 SAR of a series of bicyclic antagonists such as the 2-aminothiazolo[4,5-d]pyrimidine 3b was investigated by systematic variation of the fused pyrimidine-based heterocyclic cores. Replacement of the aminothiazole ring with a 2-thiazolone alternative led to a series of thiazolo[4,5-d]pyrimidine-2(3H)-one antagonists with markedly improved biological and pharmacokinetic properties, which are suitable pharmacological tools to probe the in vivo effects of CXCR2 antagonism combined with the associated CCR2 activity.

journal_name

Bioorg Med Chem Lett

authors

Walters I,Austin C,Austin R,Bonnert R,Cage P,Christie M,Ebden M,Gardiner S,Grahames C,Hill S,Hunt F,Jewell R,Lewis S,Martin I,David Nicholls,David Robinson

doi

10.1016/j.bmcl.2007.11.039

subject

Has Abstract

pub_date

2008-01-15 00:00:00

pages

798-803

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01348-0

journal_volume

18

pub_type

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