Synthesis and antibacterial activity of 5-methylphenanthridium derivatives as FtsZ inhibitors |
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| Authors: | Fang Liu Henrietta Venter Fangchao Bi Susan J. Semple Jingru Liu Chaobin Jin Shutao Ma |
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| Affiliation: | 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, PR China;2. School of Pharmacy & Medical Sciences, Sansom Institute for Health Research, University of South Australia, GPO Box 2471, Adelaide 5001, Australia |
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| Abstract: | 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 4 µg/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. |
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| Keywords: | Antimicrobials Biological evaluation FtsZ Structure-activity relationships 5-Methylphenanthridium derivatives |
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