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

作者：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

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(23): 6950-6954.

DOI：10.1016/j.bmcl.2011.09.133

• CCR5
• Chemokine receptor
• HIV-1
• Schering C

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 alpha-glycoprotein were evaluated in rat and dog pharmacokinetics.

• 出版日期2011-12-1
• 单位河北医科大学