Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency

…, A Liauw, Z Wang, G Emmett, DA Wacker…

Index: De Lucca, George V.; Ui, Tae Kim; Vargo, Brian J.; Duncia, John V.; Santella III, Joseph B.; Gardner, Daniel S.; Zheng, Changsheng; Liauw, Ann; Wang, Zhang; Emmett, George; Wacker, Dean A.; Welch, Patricia K.; Covington, Maryanne; Stowell, Nicole C.; Wadman, Eric A.; Das, Anuk M.; Davies, Paul; Yeleswaram, Swamy; Graden, Danielle M.; Solomon, Kimberly A.; Newton, Robert C.; Trainor, George L.; Decicco, Carl P.; Ko, Soo S. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2194 - 2211

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Citation Number: 59

Abstract

Starting with our previously described20 class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The resulting compound, 32, is a potent and selective antagonist of CCR3. SAR studies showed that the 3- acetylphenyl urea of 32 could be replaced with heterocyclic ureas or heterocyclic- ...