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Tuning the biological activity of cationic anthraquinone analogues specifically toward Staphylococcus aureus.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2018 Sep 05; Vol. 157, pp. 683-690. Date of Electronic Publication: 2018 Aug 06. - Publication Year :
- 2018
-
Abstract
- Development of new antibacterial agents against drug resistant bacteria is an imminent task, especially against methicillin-resistant Staphylococcus aureus (MRSA). While MRSA can still be treated with broad spectrum antibiotics, the use of which often leads to the disruption of normal microbial flora leading to Clostridium difficile infection (CDI). Herein, a new class of antibacterial agent, cationic anthraquinone analogues specifically against MRSA, has been developed. Through the variation and optimization of substituents, these agents are selective toward MRSA, and not Gram negative bacteria which may avoid the problem of CDI. In addition, newly discovered lead compounds also show significantly reduced cytotoxicity against normal mammalian cells than cancerous cells. This interesting finding can alleviate the toxicity and side effect problems often associate with the use of antibiotics.<br /> (Copyright © 2018 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Anthraquinones chemical synthesis
Anthraquinones chemistry
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Cations chemical synthesis
Cations chemistry
Cations pharmacology
Cell Line
Cell Survival drug effects
Dose-Response Relationship, Drug
Humans
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship
Anthraquinones pharmacology
Anti-Bacterial Agents pharmacology
Methicillin-Resistant Staphylococcus aureus drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 157
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 30130717
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.08.018