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Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
A macrolactone from benzo[a]phenazine with potent activity against Mycobacterium tuberculosis
Raphael S F Silva1, Maria do Carmo F R Pinto, Marília O F Goulart
1Núcleo de Pesquisas de Produtos Naturais, CCS, Universidade Federal do Rio de Janeiro, Ilha do Fundão, 21941-902 Rio de Janeiro, RJ, Brazil.
Abstract:
We report here an alternative to the MCPBA or ozonolysis-based oxidation methods of quinoxaline-featuring compounds prepared from beta-lapachones. The use of peracetic acid allowed a simple preparation of the corresponding macrolactones by cleavage of the ring system. These lactones were evaluated for their antimycobacterial potential and compound 4 turned out to have an MIC of 0.62 microg per mL on Mycocabteriumtuberculosis H37Rv. These results justify further research into its value as a potential lead for an original treatment of tuberculosis.
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