Abstract
Objective: the development of new drugs against Methicillin-resistant Staphylococcus aureus is a priority to the World Health Organization. So, the objective of this study was to evaluate the antibacterial activity and toxicity of 5-bromo-3-((4-methoxyphenyl) sulfenyl)-1H-indole (3b) against MRSA.Methods: minimum inhibitory concentration (MIC) of 3b was determined against S. aureus ATCC 29213 and 43 clinical isolates. The time-kill assay was performed for 9 isolates. Analysis of variance followed by the post hoc Bonferroni test was used for the statistical tests.Results and conclusions: the MIC50 and MIC90 of 3b were 4 μg.mL-1 and 16 μg.mL-1 respectively. In time-kill assay, the 3b showed bactericidal activity to all evaluated isolates at concentrations of 1xMIC and 2xMIC and the re-growth effect was not observed. About the toxicity tests, 3b has not presented cytotoxicity, mutagenicity, or allergenicity. 3b had particularly good activity against MRSA demonstrating high potential for the development of new antimicrobials products.
Reference19 articles.
1. Word Heath Organization. Global priority list of antibiotic- resistant bacteria to guide research, discovery, and development of new antibiotics [Internet]; 2017 [cited 2017 Nov 20]. Available from: http://www.who.int/medicines/publications/global-prioty-list-antibiotic-resistant-bacteria
2. Moellering RC. Discovering new antimicrobial agents. Int J Antimicrob Agents. 2011;37(1):2-9. https://doi.org/10.1016/j.ijantimicag.2010.08.018
3. Welsch ME, Snyder, Stockwell BR. Privileged scaffolds for library design and drug Discovery. Curr Opin Chem Bio. 2010;14(3):347-61. https://doi.org/10.1016/j.cbpa.2010.02.018
4. Batista BG, Lana DFD, Silveira GP, Sá MM, Ferreira M, Russo TVC, et al. Allylic selenocyanate as new agents to combat Fusarium species involved with human infections. Chemistry Select. 2017;2(35):11926-32. https://doi.org/10.1002/slct.201702338
5. Azeredo JB, Godoi M, Martins GM, Silveira CC, Braga AL. A solvent- and metal-free synthesis of 3‑Chacogenyl- indoles employing DMSO/I2 as an eco-friendly catalytic oxidation system. J Org Chem. 2014;79(9):4125-50. https://doi.org/10.1021/jo5000779
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献