Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells.

A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of RANTES binding and these compounds exhibited potent inhibition of HIV-1 replication in peripheral blood mononuclear cells.Figure optionsDownload as PowerPoint slide