| Literature DB >> 18240390 |
Iain Walters1, Caroline Austin, Rupert Austin, Roger Bonnert, Peter Cage, Mark Christie, Mark Ebden, Stuart Gardiner, Caroline Grahames, Steven Hill, Fraser Hunt, Robert Jewell, Shirley Lewis, Iain Martin.
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.Entities:
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Year: 2008 PMID： 18240390 DOI： 10.1016/j.bmcl.2007.11.039
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823