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

Rani Anu; Viljoen Albertus; Johansen Matt D.; Kremer Laurent; Kumar Vipan

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

机译：通过烷基/酰胺接头偶联的取代的异吲哚-1,3-二酮-4-氨基喹啉的合成，抗分枝杆菌和细胞毒性评价

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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.

机译：通过微波加热制备一系列仲胺取代的异吲哚-1,3-二酮-4-氨基喹啉，并测定其抗分枝杆菌活性。作为两种药物团和哌啶之间的丁基链作为异胺组分的丁基链的化合物是合成化合物中最有效和非细胞毒性的，表现出6.25μgmm的最小抑制浓度（Mic99）（-1）针对结核分枝杆菌。

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《RSC Advances》 |2019年第15期|共14页
作者
Rani Anu; Viljoen Albertus; Johansen Matt D.; Kremer Laurent; Kumar Vipan;
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Guru Nanak Dev Univ Dept Chem Amritsar 143005 Punjab India;

Univ Montpellier Inst Rech Infectiol IRIM Montpellier CNRS UMR 9004 Montpellier France;

Univ Montpellier Inst Rech Infectiol IRIM Montpellier CNRS UMR 9004 Montpellier France;

Univ Montpellier Inst Rech Infectiol IRIM Montpellier CNRS UMR 9004 Montpellier France;

Guru Nanak Dev Univ Dept Chem Amritsar 143005 Punjab India;

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正文语种 eng
中图分类化学;
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1. Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled via alkyl/amide linkers [J] . Rani Anu, Viljoen Albertus, Johansen Matt D., RSC Advances . 2019,第15期

机译：通过烷基/酰胺接头偶联的取代的异吲哚-1,3-二酮-4-氨基喹啉的合成，抗分枝杆菌和细胞毒性评价
2. Synthesis of 3-Isopropylbenzo[D]Oxazol-2(3H)-One Amides and UreaDerivatives; Evaluation of their Anti-Mycobacterial and Cytotoxic Activity [J] . Indrasena Reddy K, Aruna C, Padma Sridevi J, Medicinal Chemistry . 2017,第5期

机译：3-异丙基苯并[D] Oxazol-2（3H）-1酰胺和脲衍生物的合成;评估其抗分枝杆菌和细胞毒活性
3. Synthesis, Molecular Docking and Cytotoxicity Evaluation of 2-(4-Substituted-Benzyl) Isoindoline-1, 3-Dione Deriva-Tives as Anticancer Agents [J] . Alireza Aliabadi, Alireza Foroumadi, Maliheh Safavi, Journal of Reports in Pharmaceutical Sciences . 2012,第1期

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

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