Antibacterial activity of substituted 5-methylbenzo[c]phenanthridinium derivatives

被引：36

作者：

Parhi, Ajit ^{[2
]}

Kelley, Cody ^{[1
]}

Kaul, Malvika ^{[3
]}

Pilch, Daniel S. ^{[3
]}

LaVoie, Edmond J. ^{[1
]}

机构：

[1] Rutgers State Univ, Dept Med Chem, Piscataway, NJ 08854 USA

[2] TAXIS Pharmaceut Inc, N Brunswick, NJ 08902 USA

[3] Univ Med & Dent New Jersey, Robert Wood Johnson Med Sch, Dept Pharmacol, Piscataway, NJ 08854 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 23期

关键词：

Benzo[c]phenanthridine; FtsZ-targeting; Staphylococcus aureus; Enterococcus faecalis; CELL-DIVISION; FTSZ; INHIBITORS;

D O I：

10.1016/j.bmcl.2012.09.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Antibiotic resistance has prompted efforts to discover antibiotics with novel mechanisms of action. FtsZ is an essential protein for bacterial cell division, and has been viewed as an attractive target for the development of new antibiotics. Sanguinarine is a benzophenanthridine alkaloid that prevents cytokinesis in bacteria by inhibiting FtsZ self-assembly. In this study, a series of 5-methylbenzo[c]phenanthridinium derivatives were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and Enterococcus faecalis. The data indicate that the presence of a 1- or 12-phenyl substituent on 2,3,8,9-tetramethoxy-5-methylbenzo[c]phenanthridinium chloride significantly enhances antibacterial activity relative to the parent compound or sanguinarine. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7080 / 7083

页数：4

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