Synthesis and antibacterial activity of 5-methylphenanthridium derivatives as FtsZ inhibitors
| Autor: | Jingru Liu, Fang Liu, Shutao Ma, Henrietta Venter, Fangchao Bi, Susan J. Semple, Chaobin Jin |
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| Přispěvatelé: | Liu, Fang, Venter, Henrietta, Bi, Fangchao, Semple, Susan J, Liu, Jingrui, Jin, Chaobin, Ma, Shutao |
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Stereochemistry Streptococcus pyogenes 030106 microbiology Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests FtsZ Biochemistry antimicrobials 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship 5-methylphenanthridium derivatives Bacterial Proteins Drug Discovery Side chain Sanguinarine Molecular Biology Alkyl chemistry.chemical_classification biology Dose-Response Relationship Drug Molecular Structure Chemistry structure-activity relationships Organic Chemistry biological evaluation biology.organism_classification Antimicrobial In vitro Anti-Bacterial Agents Phenanthridines Cytoskeletal Proteins 030104 developmental biology biology.protein Molecular Medicine Antibacterial activity Bacteria Bacillus subtilis |
| Zdroj: | Bioorganicmedicinal chemistry letters. 27(15) |
| ISSN: | 1464-3405 |
| Popis: | 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. Refereed/Peer-reviewed |
| Databáze: | OpenAIRE |
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