GSK2200150A is identified by high-throughput screening (HTS) campaign that can be used as an anti-tuberculosis (TB) agent (MIC = 0.38 ?M).
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GSK2200150A is identified by high-throughput screening (HTS) campaign that can be used as an anti-tuberculosis (TB) agent (MIC = 0.38 ?M).
GSK2200150A is a novel antimycobacterial agent against Mycobacterium tuberculosis, by inhibiting the growth of virulent M.tuberculosis strain (H37Rv) with MIC of 0.38 μM.[1]
[1] Badiola KA, et al. PLoS One. 2014 Dec 10;9(12):e111782.
Cell experiment: | GSK2200150A is tested for activity at either single concentration (100 μM) or serially diluted in 10 μL of purified H2O in triplicate in 96 well microtiter plates. M. tuberculosis H37Rv is grown in complete Middlebrook 7H9 media containing albumin, dextrose and catalase (ADC), 20% Tween 80 and 50% glycerol. A bacterial suspension (90 μL) at OD600 nm of 0.001 is added to the wells and incubated for 7 days. Resazurin (10 μL; 0.05%(w/v)) is then added, incubated for 24 h at 37°C, and fluorescence measured at 590 nm using a FLUOstar Omega microplate reader. After subtraction of background fluorescence from all wells, the percentage mycobacterial survival is determined by comparing the fluorescence of wells containing compounds compared to control wells not treated with compound[1]. |
参考文献: [1]. Badiola KA, et al. Efficient Synthesis and Anti-Tubercular Activity of a Series of Spirocycles: An Exercise in OpenScience. PLoS One. 2014 Dec 10;9(12):e111782. |
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