Synergistic Effects Between Thioxanthones and Oxacillin Against Methicillin-Resistant Staphylococcus aureus

Microbial Drug Resistance : MDR : Mechanisms, Epidemiology, and Disease
Lucinda J BessaPaulo Martins da Costa

Abstract

The extensive use of antimicrobials is leaving medicine with few effective therapeutic options to treat many infections due to the fact that many organisms developed resistance to commonly used drugs. It is therefore pertinent to search not only for new antimicrobials but also for compounds able to restore or potentiate the activity of existing antibiotics. We have screened a library consisting of 40 (thio)xanthone derivatives for antibacterial activity and possible synergistic effects when used in combination with antibiotics. Nine out of the 40 compounds exhibited antibacterial activity against Gram-positive bacteria. Two xanthone derivatives, 1-formyl-4-hydroxy-3-methoxy (7), 2-formyl-3-hydroxy-4-methoxyxanthone (8) and the thioxanthone derivative 1-((2-(diethylamino)ethyl)amino)-4-propoxythioxanthone (10) and its hydrochloride form 13, showed activity against a methicillin-resistant Staphylococcus aureus (MRSA) isolate with minimum inhibitory concentration (MIC) values lower than 256 μg/ml. Thioxanthone 10 demonstrated antibacterial activity and also synergy when combined with ampicillin and oxacillin against MRSA. Additionally, thioxanthone 1-(piperidin-1-yl)-4-propoxythioxanthone (9), despite not having antibacterial acti...Continue Reading

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Citations

Jul 26, 2016·Frontiers in Microbiology·Ana P Sant'Anna da SilvaVera L de Menezes Lima
Oct 17, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Diana I S P ResendeMadalena M M Pinto
May 28, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Diana I S P ResendeMadalena M M Pinto
Nov 21, 2020·Future Microbiology·Lívia G do Av SáHélio Vn Júnior
Dec 8, 2020·Expert Opinion on Drug Metabolism & Toxicology·Vera SilvaRenata Silva
Jan 21, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Madalena M M PintoSara Cravo
Jun 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fernando DurãesEmília Sousa

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Methods Mentioned

BETA
NMR

Software Mentioned

Autodock Vina
HyperChem
Chemsketch
Vina
PyMOL

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