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

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Skerlj R,Bridger G,Zhou Y,Bourque E,McEachern E,Langille J,Harwig C,Veale D,Yang W,Li T,Zhu Y,Bey M,Baird I,Sartori M,Metz M,Mosi R,Nelson K,Bodart V,Wong R,Fricker S,Mac Farland R,Huskens D,Schols D

doi

10.1016/j.bmcl.2011.09.133

subject

Has Abstract

pub_date

2011-12-01 00:00:00

pages

6950-4

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01388-6

journal_volume

21

pub_type

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