Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 126, Issue -, Pages 696-704Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.12.008
Keywords
Cationic anthraquinone analogs; Triazole antibiotics; 1,4-Naphthoquinone analogs; MRSA; Multi-cationic; Quaternary ammonium compound
Categories
Funding
- NSF [CHE-1429195]
- Department of Chemistry and Biochemistry, Utah State University
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1429195] Funding Source: National Science Foundation
Ask authors/readers for more resources
A series of synthetic dimeric cationic anthraquinone analogs (CAAs) with potent antimicrobial activities against a broad range of fungi and bacteria were developed. These compounds were prepared in 2-3 steps with high overall yield and possess alkyl chain, azole, quinone, and quaternary ammonium complexes (QACs). In vitro biological evaluations reveal prominent inhibitory activities of lead compounds against several drug-susceptible and drug-resistant fungal and bacterial strains, including MRSA, VRE, Candida albicans and Aspergillus flavus. Mode of action investigation reveals that the synthesized dimeric CAA's can disrupt the membrane integrity of fungi. Computational studies reveal possible designs that can revive the activity of QACs against drug-resistant bacteria. Cytotoxicity assays in SKOV-3, a cancer cell line, show that the lead compounds are selectively toxic to fungi and bacteria over human cells. (C) 2016 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available