Hydrazines

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  • synthesis and antituberculosis activity of indole pyridine derived hydrazides hydrazide hydrazones and thiosemicarbazones
    Bioorganic & Medicinal Chemistry Letters, 2016
    Co-Authors: V S Velezheva, Albert G Kornienko, Konstantin Kazarian, B V Nikonenko, Patrick J. Brennan, Sergey E. Lyubimov, P. A. Ivanov, Konstantin Majorov
    Abstract:

    Abstract We describe the design, synthesis, and in vitro antimycobacterial activity of a series of novel simple hybrid hydrazides and hydrazide–hydrazones combining indole and pyridine nuclei. The compounds are derivatives of 1-acetylindoxyl or substituted indole-3-carboxaldehydes tethered via a hydrazine group by simple C N or double C N bonds with 3- and 4-pyridines, 1-oxide 3- and 4-pyridine carbohydrazides. The most active of 15 compounds showed MICs values against an INH-sensitive strain of Mycobacterium tuberculosis H37Rv equal to that of INH (0.05–2 μg/mL). Five compounds demonstrated appreciable activity against the INH-resistant M. tuberculosis CN-40 clinical isolate (MICs: 2–5 μg/mL), providing justification for further in vivo studies.