1,4-Naphthoquinone Analogues: Potent Antibacterial Agents and Mode of Action Evaluation.

Authors:
Palanisamy Ravichandiran
Palanisamy Ravichandiran
Key Laboratory of Material Chemistry for Energy Conversion and Storage
Sunirmal Sheet
Sunirmal Sheet
College of Agriculture and Life Sciences
Tucson | United States
Ae Rhan Kim
Ae Rhan Kim
Chonbuk National University
Dong Jin Yoo
Dong Jin Yoo
Chonbuk National University
South Korea

Molecules 2019 Apr 11;24(7). Epub 2019 Apr 11.

Department of Life Science, Department of Energy Storage/Conversion Engineering of Graduate School, and Hydrogen and Fuel Cell Research Center, Chonbuk National University, Jeollabuk-do 54896, Korea.

1,4-Naphthoquinones have antibacterial activity and are a promising new class of compound that can be used to treat bacterial infections. The goal was to improve effective antibacterial agents; therefore, we synthesized a new class of naphthoquinone hybrids, which contain phenylamino-phenylthio moieties as significant counterparts. Compound was modified as a substituted aryl amide moiety, which enhanced the antibacterial activity of earlier compounds and . In this study, five bacterial strains (), (), (), () and () were used to evaluate the antibacterial potency of synthesized naphthoquinones using the minimal inhibitory concentration (MIC) method. Most of the studied naphthoquinones demonstrated major antibacterial activity with a MIC of 15.6 µg/mL-500 µg/mL. Selected compounds (, and ) were studied for the mode of action, using intracellular ROS generation, determination of apoptosis by the Annexin V-FITC/PI assay, a bactericidal kinetic study and in silico molecular modelling. Additionally, the redox potentials of the specified compounds were confirmed by cyclic voltammetry (CV).

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Source
https://www.mdpi.com/1420-3049/24/7/1437
Publisher Site
http://dx.doi.org/10.3390/molecules24071437DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480589PMC
April 2019
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