Antibacterial activity of chalcones, hydrazones and oxadiazoles against methicillin-resistant Staphylococcus aureus

• Published in: Bioorganic & medicinal chemistry letters Vol. 22; no. 1; pp. 225 - 230
• Main Authors: Moreira Osório, Thaís, Delle Monache, Franco, Domeneghini Chiaradia, Louise, Mascarello, Alessandra, Regina Stumpf, Taisa, Roberto Zanetti, Carlos, Bardini Silveira, Douglas, Regina Monte Barardi, Célia, de Fatima Albino Smânia, Elza, Viancelli, Aline, Ariel Totaro Garcia, Lucas, Augusto Yunes, Rosendo, José Nunes, Ricardo, Smânia, Artur
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 01.01.2012; Elsevier
• Subjects: Animals; Anti-Bacterial Agents - pharmacology; Antibacterial activity; Antibacterial agents; antibacterial properties; antibiotic resistance; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Cercopithecus aethiops; Chalcones; Chalcones - chemistry; Chalcones - pharmacology; Cytotoxic activity; cytotoxicity; Humans; Hydrazones; Hydrazones - chemistry; Hydrazones - pharmacology; Medical sciences; Methicillin - pharmacology; Methicillin-Resistant Staphylococcus aureus - metabolism; Microbial Sensitivity Tests; minimum inhibitory concentration; Models, Chemical; MRSA; multiple drug resistance; Oxadiazoles; Oxadiazoles - pharmacology; pathogens; PCR and RAPD; Pharmacology. Drug treatments; Staphylococcal Infections - drug therapy; Staphylococcal Infections - microbiology; Staphylococcus aureus; Staphylococcus aureus - metabolism; Vero Cells; Chalcones; Oxadiazoles; PCR and RAPD; MRSA; Hydrazones; Antibacterial activity; Cytotoxic activity; Cytotoxicity; Flavonoid; Random amplified polymorphic DNA marker; Biological activity; Polyphenol; Phenols; Oxadiazole derivatives; Hydrazone; Antibacterial agent
• ISSN: 0960-894X; 1464-3405; 1464-3405
• DOI: 10.1016/j.bmcl.2011.11.059

Sixty-five synthetic or natural chalcones, hydrazones and oxadiazoles were assayed against Staphylococcus aureus ATCC 25923 and methicillin-resistant S. aureus (MRSA) isolates. Two chalcones, one dihydrochalcone and two hydrazones showed important activity against MRSA and are promising as antibiotic-like substances. The increase in antibiotic resistance due to multiple factors has encouraged the search for new compounds which are active against multidrug-resistant pathogens. In this context, chalcones, dihydrochalcones, hydrazones and oxadiazoles were tested against Staphylococcus aureus ATCC 25923 and methicillin-resistant S. aureus (MRSA) isolates, which were obtained from clinical laboratories and were characterized as MRSA using traditional and molecular methods. Among 65 tested compounds, two chalcones, one dihydrochalcone and two hydrazones were active against MRSA. Based on the minimal inhibitory concentration and cytotoxicity, hydrazones provided a better selectivity index than chalcones. Active hydrazones are promising antibiotic-like substances and they should be the subject of further microbiological studies.