Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled via alkyl/amide linkers

被引：10

作者：

Rani, Anu ^{[1
]}

Viljoen, Albertus ^{[2
]}

Johansen, Matt D. ^{[2
]}

Kremer, Laurent ^{[2
,3
]}

Kumar, Vipan ^{[1
]}

机构：

[1] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India

[2] Univ Montpellier, Inst Rech Infectiol IRIM Montpellier, CNRS, UMR 9004, Montpellier, France

[3] INSERM, IRIM, F-34293 Montpellier, France

来源：

RSC ADVANCES | 2019年 / 9卷 / 15期

关键词：

MEFLOQUINE-BASED LIGANDS; CONJUGATES SYNTHESIS; IN-VITRO; ANTITUBERCULOSIS; PHTHALIMIDE; ANALOGS; TUBERCULOSIS; DESIGN; MOXIFLOXACIN; INHIBITION;

D O I：

10.1039/c8ra10532d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of secondary amine-substituted isoindoline-1,3-dione-4-aminoquinolines were prepared via microwave heating and assayed for their anti-mycobacterial activities. The compound with a butyl chain as a spacer between the two pharmacophores and piperidine as the secondary amine component on the isoindoline ring was the most potent and non-cytotoxic among the synthesized compounds, exhibiting a minimum inhibitory concentration (MIC99) of 6.25 mu g mL(-1) against Mycobacterium tuberculosis.

引用

页码：8515 / 8528

页数：14

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