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An efficient and facile green synthesis of bisindole methanes as potential Mtb FtsZ inhibitors
Gayathri Ramamoorthy,
Published in Blackwell Publishing Ltd
2018
PMID: 30003661
Volume: 92
   
Issue: 6
Pages: 1933 - 1939
Abstract
The rising multidrug-resistant Mycobacterium tuberculosis (Mtb) strain made current anti-TB drug therapy ineffective and became a major health concern globally; hence it is crucial to develop new molecules against vital targets with a novel mechanism. Mtb Filamenting temperature sensitive protein Z (FtsZ), a tubulin homolog plays a major role in bacterial cell division, in the presence of GTP recruiting essential proteins for cell division and considered to be a potential target for drug discovery. Most of MtbFtsZ inhibitors known are of antibiotics from natural resources and suffer from cellular uptake, specificity. In the present study, we demonstrated for the first time bisindole derivatives as potential MtbFtsZ inhibitors. The synthesis of bisindole derivatives has been carried out using green synthetic approach by applying ammonium molybdate as a catalyst under Ultrasonic condition. Among the synthesized bisindole derivative, I16 and I5 showed 62.29% and 56.86% inhibition of GTPase activity of MtbFtsZ and increased the length of Mycobacterium smegmatis and Bacillus subtilis by two folds. Further compound I16 inhibited Mtb growth with a MIC of 37.5 μg/ml. To explain these interactions, detailed Molecular docking studies have been carried out and found to be supportive to the biological activity. © 2018 John Wiley & Sons A/S.
About the journal
JournalChemical Biology and Drug Design
PublisherBlackwell Publishing Ltd
ISSN17470277
Open AccessNo
Concepts (52)
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    ANTIMYCOBACTERIAL AGENT
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    BISINDOLE METHANE DERIVATIVE
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    FLUOROURACIL
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    Ftsz protein
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    Guanosine triphosphatase
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    Indole derivative
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    Protein inhibitor
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    Rifampicin
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    Unclassified drug
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    Bacterial protein
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    Cytoskeleton protein
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    Ftsz protein, bacteria
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    Methane
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    Tuberculostatic agent
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    Article
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    Bacillus subtilis
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    Bacterial cell
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    Bacterial growth
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    Bactericidal activity
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    Binding site
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    Catalyst
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    Cell proliferation
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    Controlled study
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    Drug synthesis
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    Enzyme activity
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    Green chemistry
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    Growth inhibition
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    In vitro study
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    Minimum inhibitory concentration
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    Molecular docking
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    Mycobacterium smegmatis
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    Mycobacterium tuberculosis
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    Nonhuman
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    Priority journal
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    REACTION DURATION (CHEMISTRY)
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    Ultrasound
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    Antagonists and inhibitors
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    Chemistry
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    Drug effect
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    Metabolism
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    MICROBIAL SENSITIVITY TEST
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    Protein tertiary structure
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    Synthesis
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    ANTITUBERCULAR AGENTS
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    Bacterial proteins
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    Binding sites
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    Cytoskeletal proteins
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    Green chemistry technology
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    Indoles
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    Microbial sensitivity tests
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    Molecular docking simulation
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    Protein structure, tertiary