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 ,
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.
