Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
4 years ago

Synthesis and antibacterial activity of 5-methylphenanthridium derivatives as FtsZ inhibitors

Synthesis and antibacterial activity of 5-methylphenanthridium derivatives as FtsZ inhibitors
5-Methylphenanthridium derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity and cell division inhibitory activity against various Gram-positive and -negative bacteria. Among them, compounds 5A2, 5B1, 5B2, 5B3, 5C1 and 5C2 displayed the best on-target antibacterial activity with an MIC value of 4µg/mL against B. subtilis ATCC9372 and S. pyogenes PS, showing over 2-fold better activity than sanguinarine. The SARs showed that the 5-methylphenanthridium derivatives with the alkyl side chains at the 2-postion, especially the straight alkyl side chains exerted better on-target antibacterial activity.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17306078

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