通过烷基/酰胺连接基连接的取代异吲哚啉-1,3-二酮-4-氨基喹啉的合成、抗分枝杆菌及细胞毒性评估
Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled alkyl/amide linkers.
作者信息
Rani Anu, Viljoen Albertus, Johansen Matt D, Kremer Laurent, Kumar Vipan
机构信息
Department of Chemistry, Guru Nanak Dev University Amritsar-143005 Punjab India
Institut de Recherche en Infectiologie (IRIM) de Montpellier, CNRS, UMR 9004 Université de Montpellier France.
出版信息
RSC Adv. 2019 Mar 13;9(15):8515-8528. doi: 10.1039/c8ra10532d. eCollection 2019 Mar 12.
A series of secondary amine-substituted isoindoline-1,3-dione-4-aminoquinolines were prepared 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) of 6.25 μg mL against .
通过微波加热制备了一系列仲胺取代的异吲哚啉-1,3-二酮-4-氨基喹啉，并对其抗分枝杆菌活性进行了测定。在合成的化合物中，以丁基链作为两个药效基团之间的间隔基且异吲哚啉环上以哌啶作为仲胺成分的化合物活性最强且无细胞毒性，对[具体菌株]的最低抑菌浓度（MIC）为6.25μg/mL。
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