N4 -benzyl-N2 -phenylquinazoline-2,4-diamine compound presents antibacterial and antibiofilm effect against Staphylococcus aureus and Staphylococcus epidermidis.
Sharon Vieira Dos ReisNicole Sartori RibeiroDébora Assumpção RochaIsadora Serraglio FortesDanielle da Silva TrentinSaulo Fernandes de AndradeAlexandre José MacedoPublished in: Chemical biology & drug design (2020)
Staphylococcus aureus and Staphylococcus epidermidis are the main agents involved with implant-related infections. Their ability to adhere to medical devices with subsequent biofilm formation is crucial to the development of these infections. Herein, we described the antibacterial and antibiofilm activities of a quinazoline-based compound, N4 -benzyl-N2 -phenylquinazoline-2,4-diamine, against both biofilm-forming pathogens. The minimum inhibitory concentrations (MIC) were determined as 25 µM for S. aureus and 15 µM for S. epidermidis. At sub-MIC concentrations (20 µM for S. aureus and 10 µM for S. epidermidis), the compound was able to inhibit biofilm formation without interfere with bacterial growth, confirmed by scanning electron microscopy. Moreover, surfaces coated with the quinazoline-based compound were able to prevent bacterial adherence. In addition, this compound presented no toxicity to human red blood cells at highest MIC 25 µM and in vivo toxicity assay using Galleria mellonella larvae resulted in 82% survival with a high dose of 500 mg/kg body weight. These features evidence quinazoline-based compound as interesting entities to promising applications in biomedical fields, such as antimicrobial and in anti-infective approaches.
Keyphrases
- biofilm formation
- staphylococcus aureus
- pseudomonas aeruginosa
- candida albicans
- escherichia coli
- electron microscopy
- body weight
- high dose
- methicillin resistant staphylococcus aureus
- endothelial cells
- red blood cell
- oxidative stress
- type diabetes
- high resolution
- low dose
- zika virus
- high throughput
- skeletal muscle
- insulin resistance
- mass spectrometry
- soft tissue
- free survival