Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor

Deka, Banani; Suri, Mrinaly; Sarma, Sangita; Moirangthem, Veigyabati Devi; Bora, Anamika; Sen, Tejosmita; Dihingia, Anjum; Pahari, Pallab; Singh, Anil Kumar

doi:10.1016/j.bmc.2021.116580

Cited by 4 publications

(2 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In sub-inhibitory concentrations, dihydroquinazoline analogs downregulated the norA gene, and when combined with norfloxacin, a 3-log reduction in the number of intracellular S. aureus in human monocytes was observed [119]. The antifungal compound ketoconazole could reduce the expression of norA, norB, and norC, resulting in an eight-fold decrease in the MIC [120].…”

Section: Downregulation Of Genes Encoding Mfs Efflux Pumpsmentioning

confidence: 99%

The Major Facilitator Superfamily and Antimicrobial Resistance Efflux Pumps of the ESKAPEE Pathogen Staphylococcus aureus

et al. 2023

View full text Add to dashboard Cite

The ESKAPEE bacterial pathogen Staphylococcus aureus has posed a serious public health concern for centuries. Throughout its evolutionary course, S. aureus has developed strains with resistance to antimicrobial agents. The bacterial pathogen has acquired multidrug resistance, causing, in many cases, untreatable infectious diseases and raising serious public safety and healthcare concerns. Amongst the various mechanisms for antimicrobial resistance, integral membrane proteins that serve as secondary active transporters from the major facilitator superfamily constitute a chief system of multidrug resistance. These MFS transporters actively export structurally different antimicrobial agents from the cells of S. aureus. This review article discusses the S. aureus-specific MFS multidrug efflux pump systems from a molecular mechanistic perspective, paying particular attention to structure–function relationships, modulation of antimicrobial resistance mediated by MFS drug efflux pumps, and direction for future investigation.

show abstract

Section: Downregulation Of Genes Encoding Mfs Efflux Pumpsmentioning

confidence: 99%

The Major Facilitator Superfamily and Antimicrobial Resistance Efflux Pumps of the ESKAPEE Pathogen Staphylococcus aureus

et al. 2023

View full text Add to dashboard Cite

show abstract

“…Of the seventeen dihydroquinazolines synthesised and screened for possible efflux pump inhibitor activity against S. aureus 1199B, eight proved to be effective inhibitors, significantly reducing the MICs of norfloxacin and ethidium bromide against S. aureus 1199B by up to 16-fold. Dihydroquinazoline analogues ( Figure 2 ) also significantly reduce norA gene expression in the presence of subinhibitory concentrations of norfloxacin [ 53 ].…”

Section: The Role Of Efflux Pump Inhibitors In Reversing Drug Resistancementioning

confidence: 99%

Bacterial Efflux Pump Inhibitors Reduce Antibiotic Resistance

Zhang,

Tian,

Sun

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

Bacterial resistance is a growing problem worldwide, and the number of deaths due to drug resistance is increasing every year. We must pay great attention to bacterial resistance. Otherwise, we may go back to the pre-antibiotic era and have no drugs on which to rely. Bacterial resistance is the result of several causes, with efflux mechanisms widely recognised as a significant factor in the development of resistance to a variety of chemotherapeutic and antimicrobial medications. Efflux pump inhibitors, small molecules capable of restoring the effectiveness of existing antibiotics, are considered potential solutions to antibiotic resistance and have been an active area of research in recent years. This article provides a review of the efflux mechanisms of common clinical pathogenic bacteria and their efflux pump inhibitors and describes the effects of efflux pump inhibitors on biofilm formation, bacterial virulence, the formation of bacterial persister cells, the transfer of drug resistance among bacteria, and mismatch repair. Numerous efforts have been made in the past 20 years to find novel efflux pump inhibitors which are known to increase the effectiveness of medicines against multidrug-resistant strains. Therefore, the application of efflux pump inhibitors has excellent potential to address and reduce bacterial resistance.

show abstract

Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections

Shinya¹,

Kawai²,

Kobayashi³

et al. 2022

Bioorganic & Medicinal Chemistry

View full text Add to dashboard Cite

Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor

Cited by 4 publications

References 39 publications

The Major Facilitator Superfamily and Antimicrobial Resistance Efflux Pumps of the ESKAPEE Pathogen Staphylococcus aureus

The Major Facilitator Superfamily and Antimicrobial Resistance Efflux Pumps of the ESKAPEE Pathogen Staphylococcus aureus

Bacterial Efflux Pump Inhibitors Reduce Antibiotic Resistance

Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections

Contact Info

Product

Resources

About