Author/Authors :
Alexander Pasternak، نويسنده , , Stephen D. Goble، نويسنده , , Pasquale P. Vicario، نويسنده , , Jerry Di Salvo، نويسنده , , Julia M. Ayala، نويسنده , , Mary Struthers، نويسنده , , Julie A. DeMartino، نويسنده , , Sander G. Mills، نويسنده , , Lihu Yang، نويسنده ,
Abstract :
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the IKr channel; poor selectivity against IKr had been a liability of earlier analogs in this series.
