Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives

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• 作者：Subhash Chander^a ; Ping Wang^b ; Penta Ashok^a ; Liu-Meng Yang^b ; Yong-Tang Zheng^b ; ^{zhengyt@mail.kiz.ac.cn} ; Murugesan Sankaranarayanan^a ; ^{murugesan@pilani.bits-pilani.ac.in}
• 关键词：Enzymatic assay ; Wild strain ; Reverse transcriptase ; Docking ; Cytotoxicity
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：61-65
• 全文大小：907 K
• 卷排序：27

文摘

Fourteen novel compounds were designed, synthesized, and evaluated for HIV-1 RT inhibition. Tested compounds displayed significant to weak potency against the selected target. Among top five RT inhibitors, four retained significant potency against HIV-1 with good safety index. Docked view of compound 7m with RT revealed prominent pi-pi stacking and hydrophobic interaction.