Title of article
Evaluation of a series of bicyclic CXCR2 antagonists
Author/Authors
Iain Walters، نويسنده , , Caroline Austin، نويسنده , , Rupert Austin، نويسنده , , Roger Bonnert، نويسنده , , Peter Cage، نويسنده , , Mark Christie، نويسنده , , Mark Ebden، نويسنده , , Stuart Gardiner، نويسنده , , Caroline Grahames، نويسنده , , Steven Hill، نويسنده , , Fraser Hunt، نويسنده , , Robert Jewell، نويسنده , , Shirley Lewis، نويسنده , , Iain Martin، نويسنده , , David Nicholls، نويسنده , , David Robinson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
798
To page
803
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.
Keywords
CXCR2 , 5-d]pyrimidine-2(3H)-one
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799062
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