Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
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DOI：
10.1371/journal.pone.0053636
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发表时间：
2013
期刊：
影响因子：
3.7
通讯作者：
Hu Y
中科院分区：
文献类型：
--
作者：
Liu T;Weng Z;Dong X;Chen L;Ma L;Cen S;Zhou N;Hu Y
利用片段组装策略和生物等构置换原理，设计、合成了一系列新型哌嗪衍生物，并对其细胞靶效应器融合活性和体外抗病毒活性进行了评价。本研究初步总结了目标化合物的构效关系，发现5个化合物在低微摩尔水平下具有中等至强的CCR5融合活性，IC50值为低微摩尔水平。在被评估的化合物中，23 h被发现是CCR5拮抗剂，IC50值为6.29µM，抗hiv -1抑制剂的IC50值为0.44µM。
By using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relationships (SARs) of target compounds were concluded in this study, and five compounds were found to exhibited medium to potent CCR5 fusion activities with IC50 values in low micromolar level. Among evaluated compounds, 23 h was found to be a CCR5 antagonist with an IC50 value of 6.29 µM and an anti-HIV-1 inhibitor with an IC50 value of 0.44 µM.
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