372156-99-5Relevant articles and documents
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication
Skerlj, Renato,Bridger, Gary,Zhou, Yuanxi,Bourque, Elyse,McEachern, Ernest,Langille, Jonathan,Harwig, Curtis,Veale, Duane,Yang, Wen,Li, Tongshong,Zhu, Yongbao,Bey, Michael,Baird, Ian,Sartori, Michael,Metz, Markus,Mosi, Renee,Nelson, Kim,Bodart, Veronique,Wong, Rebecca,Fricker, Simon,Mac Farland, Ron,Huskens, Dana,Schols, Dominique
, p. 6950 - 6954 (2012/01/13)
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics.
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
Palani,Shapiro,Clader,Greenlee,Cox,Strizki,Endres,Baroudy
, p. 3339 - 3342 (2007/10/03)
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 (Ki=2 nM), which possesses subnanomolar activity in blocking viral entry and