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Novel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine

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dc.contributor.authorLiu, J.
dc.contributor.authorMa, R.
dc.contributor.authorBi, F.
dc.contributor.authorZhang, F.
dc.contributor.authorHu, C.
dc.contributor.authorVenter, H.
dc.contributor.authorSemple, S.J.
dc.contributor.authorMa, S.
dc.date.issued2018
dc.description.abstractA novel series of 5-methyl-2-phenylphenanthridium derivatives were displayed outstanding activity against a panel of antibiotic-sensitive and -resistant bacteria strains compared with their precursor sanguinarine, ciprofloxacin and oxacillin sodium. Compounds 7 l, 7m and 7n were found to display the most effective activity against five sensitive strains (0.06–2 μg/mL) and three resistant strains (0.25–4 μg/mL). The kinetic profiles indicated that compound 7l possessed the strongest bactericidal effect on S. aureus ATCC25923, with the MBC value of 16 μg/mL. The cell morphology and the FtsZ polymerization assays indicated that these compounds inhibited the bacterial proliferation by interfering the function of bacterial FtsZ. The SARs showed that all the 4-methyl-substituted 5-methyl-2-phenylphenanthridium subseries could be further investigated as the FtsZ-targeting antibacterial agents.
dc.identifier.citationBioorganic and Medicinal Chemistry Letters, 2018; 28(10):1825-1831
dc.identifier.doi10.1016/j.bmcl.2018.04.015
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.urihttps://hdl.handle.net/11541.2/131786
dc.language.isoen
dc.publisherPergamon Press
dc.rightsCopyright 2018 Published by Elsevier
dc.source.urihttps://doi.org/10.1016/j.bmcl.2018.04.015
dc.subjectantibacterial activity
dc.subjectFtsZ-targetingantibacterial agents
dc.subjectderivatives
dc.subject5-Methyl-2-phenylphenanthridium
dc.titleNovel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine
dc.typeJournal article
pubs.publication-statusPublished
ror.mmsid9916188203401831

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