Author/Authors :
Mingde Xia، نويسنده , , Cuifen Hou، نويسنده , , Scott Pollack، نويسنده , , James Brackley، نويسنده , , Duane DeMong، نويسنده , , Meng Pan، نويسنده , , Monica Singer، نويسنده , , Michele Matheis، نويسنده , , Gil Olini، نويسنده , , Druie Cavender، نويسنده , , Michael Wachter، نويسنده ,
Abstract :
A series of phenyl piperidine derivatives possessing potent and selective CCR2 antagonist activity is reported. Structure–activity relationship (SAR) studies have established that incorporation of a second ring system adjacent to the aryl piperidine plays an important role in determining the CCR2 potency. Both a second piperidine ring and a 1,3-substituted cyclopentylamine have been probed as linkers. For the cyclopentylamine series, the 1S,3R-configuration exhibits much higher affinity for hCCR2 than the 1R,3S-configuration. Compound 3g shows good selectivity over CCR1, CCR3, 5-HT and has an excellent P450 profile.
