Discovery of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl- 3pyridinyl)carbonyl]-4′-methyl-1,4′bipiperidine N-oxide (SCH 351125): An orally bioavailable human CCR5 antagonist for the treatment of HIV infection

Article abstract of DOI:10.1021/jm015526o

Structure - activity studies on piperidino-piperidine 3 led to the discovery of SCH 351125 (1), a selective CCR5 antagonist with potent activity against RANTES binding (K_i=2 nM), which possesses subnanomolar activity in blocking viral entry and