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


ABSTRACT: 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 μg mL-1 against Mycobacterium tuberculosis.

SUBMITTER: Rani A 

PROVIDER: S-EPMC9061829 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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

Rani Anu A   Viljoen Albertus A   Johansen Matt D MD   Kremer Laurent L   Kumar Vipan V  

RSC advances 20190313 15


A series of secondary amine-substituted isoindoline-1,3-dione-4-aminoquinolines were prepared <i>via</i> 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 (MIC<sub>99</sub>) of 6.25 μg mL<sup>-1</sup> against <i>Myc  ...[more]

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