Author/Authors :
Jayaram R. Tagat، نويسنده , , Stuart W. McCombie، نويسنده , , Ruo W. Steensma، نويسنده , , Sue-Ing Lin، نويسنده , , Dennis V. Nazareno، نويسنده , , Bahige Baroudy، نويسنده , , Nicole Vantuno، نويسنده , , Serena Xu، نويسنده , , Jia Liu، نويسنده ,
Abstract :
Optimization of the piperidino-piperazines 1 and 2 provided early leads 3 and 4, which showed good activity in the CCR5–RANTES binding assay and in antiviral assays. A systematic study around these structures showed that the 2(S)-methyl piperazine is essential for CCR5 affinity, which is further enhanced by forming the 2,6-dimethyl benzamide of the piperidine.
