设计和合成吡啶-2-基甲基氨基哌啶-1-基丁基酰胺 CCR5 拮抗剂，其对 M 嗜性（R5）HIV-1 复制具有强效抑制作用。
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
机构信息
Genzyme Corp., 153 Second Avenue, Waltham, MA 02451, USA.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):6950-4. doi: 10.1016/j.bmcl.2011.09.133. Epub 2011 Oct 8.
PMID:22033460
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.
摘要
一系列 CCR5 拮抗剂被优化以强效抑制外周血单核细胞中的 R5 HIV-1 复制。符合可接受的 ADME 标准、选择性、人血浆蛋白结合、在 α-糖蛋白存在下效力改变的化合物在大鼠和狗的药代动力学中进行了评估。
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