Evaluation of the Efflux Pump Inhibition Activity of Thiadiazine-Derived Compounds Against the Staphylococcus aureus 1199B Strain
Cicera Laura Roque Paulo, Priscilla Ramos Freitas Alexandre, Ana Carolina Ferreira Araujo, Ray Silva Almeida, Emílio Sousa Albuquerque, Cícera Datiane de Morais Oliveira-Tintino, Igor J. S. Nascimento, João Xavier Araújo-Júnior, Edeildo Ferreira da Silva-Junior
TL;DR
This study evaluates thiadiazine-derived compounds for their ability to inhibit bacterial efflux pumps and combat drug-resistant Staphylococcus aureus.
Contribution
The study introduces thiadiazine-derived compound IJ28 as a promising efflux pump inhibitor against multidrug-resistant Staphylococcus aureus.
Findings
Compound IJ28 showed direct antibacterial activity with an MIC of 512 µg/mL against Staphylococcus aureus 1199B.
IJ28 significantly reduced the MIC of ethidium bromide from 26.6 µg/mL to 0.5 µg/mL, indicating efflux pump inhibition.
In silico and fluorescence tests confirmed IJ28's potential as an efflux pump inhibitor.
Abstract
Background: Substances with antibacterial properties have become crucial in light of the continuous increase in infections caused by multidrug-resistant bacteria. In this context, thiadiazines have emerged as heterocyclic compounds already known for their pharmacological activities. However, their potential as antibacterial agents and inhibitors of the efflux system found in resistant bacteria remains poorly understood. From this perspective, the present study highlights the synthesis of thiadiazine-derived compounds and evaluates their antibacterial activity and efflux pump inhibition against the Staphylococcus aureus 1199B strain. Methods: To this end, Minimum Inhibitory Concentration (MIC) tests were conducted, along with the analysis of antibacterial activity through the inhibition of the NorA efflux system using 96-well microdilution assays. Additionally, to assess efflux system…
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Taxonomy
TopicsPhenothiazines and Benzothiazines Synthesis and Activities · Synthesis and biological activity · Quinazolinone synthesis and applications