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Benzaldehyde thiosemicarbazone derivatives against replicating and nonreplicating Mycobacterium tuberculosis.
Volynets, Galyna P; Tukalo, Michail A; Bdzhola, Volodymyr G; Derkach, Nataliia M; Gumeniuk, Mykola I; Tarnavskiy, Sergiy S; Starosyla, Sergiy A; Yarmoluk, Sergiy M.
Afiliación
  • Volynets GP; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine. galina.volinetc@gmail.com.
  • Tukalo MA; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine.
  • Bdzhola VG; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine.
  • Derkach NM; National Institute of Phthisiology and Pulmonology named after F.G. Yanovsky, NAMS of Ukraine, 10, M. Amosova Street, 03038, Kyiv, Ukraine.
  • Gumeniuk MI; National Institute of Phthisiology and Pulmonology named after F.G. Yanovsky, NAMS of Ukraine, 10, M. Amosova Street, 03038, Kyiv, Ukraine.
  • Tarnavskiy SS; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine.
  • Starosyla SA; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine.
  • Yarmoluk SM; Institute of Molecular Biology and Genetics, NAS of Ukraine, 150 Zabolotnogo Street, 03143, Kyiv, Ukraine.
J Antibiot (Tokyo) ; 72(4): 218-224, 2019 04.
Article en En | MEDLINE | ID: mdl-30662064
In this article, we report a series of benzaldehyde thiosemicarbazone derivatives possessing high activity toward actively replicating Mycobacterium tuberculosis strain with minimum inhibitory concentration (MIC) values in the range from 0.14 to 2.2 µM. Among them, two compounds-2-(4-phenethoxybenzylidene)hydrazine-1-carbothioamide (13) and 2-(3-isopropoxybenzylidene)hydrazine-1-carbothioamide (20) also demonstrate submicromolar antimycobacterial activity against M. tuberculosis under hypoxia with MIC values of 0.68 and 0.74 µM, respectively. The activity of compounds 13 and 20 toward five investigated isoniazid-, rifampicin-, and fluoroquinolone-resistant M. tuberculosis isolates is similar to commercially available antituberculosis drugs. The compounds 13 and 20 possess good ADME properties and have low cytotoxicity toward human liver cells (HepG2). Therefore, 2-(4-phenethoxybenzylidene)hydrazine-1-carbothioamide (13) and 2-(3-isopropoxybenzylidene)hydrazine-1-carbothioamide (20) are valuable candidates for further preclinical studies.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiosemicarbazonas / Benzaldehídos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: J Antibiot (Tokyo) Año: 2019 Tipo del documento: Article País de afiliación: Ucrania Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiosemicarbazonas / Benzaldehídos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: J Antibiot (Tokyo) Año: 2019 Tipo del documento: Article País de afiliación: Ucrania Pais de publicación: Reino Unido