Quinonoid and phenazine compounds: synthesis of new antimycobacterial prototypes

Proceedings of the 14th Brazilian Meeting on Organic Synthesis Proceedings(2013)

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摘要
The minimum inhibitory concentrations (MICs) for the compounds were evaluated against MT H37Rv, MT rifampicin resistance (ATCC 35338) and MT isoniazid resistance (ATCC 35822). The toxicity of compounds toward a normal proliferating cell was investigated using the Alamar Blue assay. The compounds were classified by us according to their activity against MT as highly active (MIC ≤ 3 μg/mL), lowly active (3 μg/mL 100 μg/mL). Lapachol (1) and the compounds 2, 9 and 10, were considered inactive when MIC >100 μg/mL for H37Rv, ATCC 35338 and ATCC 35822 strains and the substances 3 and 4 were lowly active. With MIC value of 25, 12.5 and 25 μg/mL for MT H37Rv, MT rifampicin resistance and MT isoniazid resistance the reduced quinone 4 can be considered as an important prototype. The substance 7 was highly active [MIC ≤ 3 μg/mL (9.75 μM)] against MT H37Rv. For ATCC 35822 strains the compound was less active with MIC value of 12.5 μg/mL and for ATCC 35822 strain was inactive. The substance 7 was not cytotoxic against normal cells (IC50 > 25 μg/mL).
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synthesis,compounds
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