N 4 ‐benzyl‐N 2 ‐phenylquinazoline‐2,4‐diamine compound presents antibacterial and antibiofilm effect against Staphylococcus aureus and Staphylococcus epidermidis

Autor:	Nicole Sartori Ribeiro, Isadora Serraglio Fortes, Débora Assumpção Rocha, Sharon Vieira dos Reis, Saulo Fernandes de Andrade, Danielle da Silva Trentin, Alexandre José Macedo
Rok vydání:	2020
Předmět:	Pharmacology biology 010405 organic chemistry Chemistry Organic Chemistry Biofilm Bacterial growth biology.organism_classification Antimicrobial medicine.disease_cause 01 natural sciences Biochemistry 0104 chemical sciences Microbiology Galleria mellonella 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Staphylococcus epidermidis Staphylococcus aureus Drug Discovery Toxicity medicine Quinazoline Molecular Medicine
Zdroj:	Chemical Biology & Drug Design. 96:1372-1379
ISSN:	1747-0285 1747-0277
DOI:	10.1111/cbdd.13745
Popis:	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.
Databáze:	OpenAIRE
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