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Synthesis and antituberculosis activity of indole-pyridine derived hydrazides, hydrazide-hydrazones, and thiosemicarbazones.
Velezheva, Valeriya; Brennan, Patrick; Ivanov, Pavel; Kornienko, Albert; Lyubimov, Sergey; Kazarian, Konstantin; Nikonenko, Boris; Majorov, Konstantin; Apt, Alexander.
Afiliación
  • Velezheva V; A.N.Nesmeyanov Institute of Organoelement Compounds Russian Academy of Sciences, 28 Vavilov Str., 117813 Moscow, Russia.
  • Brennan P; Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, CO 80523-1682 USA.
  • Ivanov P; A.N.Nesmeyanov Institute of Organoelement Compounds Russian Academy of Sciences, 28 Vavilov Str., 117813 Moscow, Russia.
  • Kornienko A; A.N.Nesmeyanov Institute of Organoelement Compounds Russian Academy of Sciences, 28 Vavilov Str., 117813 Moscow, Russia.
  • Lyubimov S; A.N.Nesmeyanov Institute of Organoelement Compounds Russian Academy of Sciences, 28 Vavilov Str., 117813 Moscow, Russia.
  • Kazarian K; Central TB Research Institute Russian Academy of Medical Sciences, 2, Yauzskaya Alley, 107564 Moscow, Russia.
  • Nikonenko B; Central TB Research Institute Russian Academy of Medical Sciences, 2, Yauzskaya Alley, 107564 Moscow, Russia.
  • Majorov K; Central TB Research Institute Russian Academy of Medical Sciences, 2, Yauzskaya Alley, 107564 Moscow, Russia.
  • Apt A; Central TB Research Institute Russian Academy of Medical Sciences, 2, Yauzskaya Alley, 107564 Moscow, Russia.
Bioorg Med Chem Lett ; 26(3): 978-985, 2016 Feb 01.
Article en En | MEDLINE | ID: mdl-26725953
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiosemicarbazonas / Hidrazinas / Hidrazonas / Antituberculosos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Rusia Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiosemicarbazonas / Hidrazinas / Hidrazonas / Antituberculosos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Rusia Pais de publicación: Reino Unido