Design and synthesis of pyridin-2-yloxymethylpiperidin-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; Langille Jonathan; Di Fluri Maria; Bogucki David; Yang Wen; Li Tongshuang; Wang Letian; Nan Susan; Baird Ian; Metz Markus; Darkes Marilyn; Labrecque Jean; Lau Gloria; Fricker Simon; Huskens Dana; Schols Dominique

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(8): 2450-2455.

DOI：10.1016/j.bmcl.2011.02.058

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

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.

• 出版日期2011-4-15
• 单位河北医科大学