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Heteronuclear 5‐Fluoroisatin Dimers: Design, Synthesis, and Evaluation of Their In Vitro Anti‐mycobacterial Activities
Author(s) -
Deng JiaLun,
Liu XiaoCheng,
Cai GuangWei,
Zhang Gang,
Hu Li,
Qiu Li,
Li ZiYong,
Xu Zhi
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3186
Subject(s) - heteronuclear molecule , mycobacterium tuberculosis , chemistry , rifampicin , isoniazid , in vitro , minimum inhibitory concentration , tuberculosis , stereochemistry , microbiology and biotechnology , antibiotics , biochemistry , nuclear magnetic resonance spectroscopy , medicine , biology , pathology
A series of novel heteronuclear 5‐fluoroisatin dimers 4a–j tethered through ethylene were designed, synthesized, and examined for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H37Rv and multi‐drug resistant tuberculosis (MDR‐TB). All hybrids exhibited potential anti‐mycobacterial activities against the tested two strains with minimum inhibitory concentration (MIC) in a range of 25 to 256 μg/mL. In particular, the heteronuclear 5‐fluoroisatin dimer 4a (MIC: 25 and 32 μg/mL) was most active against Mycobacterium tuberculosis H37Rv and MDR‐TB strains, which was twofold and greater than fourfold more potent than rifampicin (MIC: 64 μg/mL) and isoniazid (MIC: >128 μg/mL) against MDR‐TB, warrant further optimization.