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System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
In Vitro Activity of 3-Triazeneindoles against Mycobacterium tuberculosis and Mycobacterium avium
Boris V Nikonenko1, Albert Kornienko2, Konstantin Majorov3
1Central Institute for Tuberculosis, Moscow, Russia TB-Stopper, Skolkovo, Moscow, Russia b.nikonenko@mail.ru.
Abstract:
Among 230 target-synthesized indole-based compounds, seven 3-triazenoindoles showed MICs of 0.2 to 0.5 μg/ml against Mycobacterium tuberculosis strain H37Rv and isoniazid-resistant human isolate CN-40. The TU112 compound was active also against a dormant form of M. tuberculosis Some of these triazenoindoles were active against Mycobacterium avium, with MICs of 0.05 to 0.5 μg/ml. The selectivity indices (SI) for M. tuberculosis and M. avium were significantly higher than 10, making these compounds acceptable for the next testing step.
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