Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents
Тип публікації :
Стаття
Дата випуску :
2015
Автор(и) :
Menendez, Christophe
Mori, Giorgia
Maillot, Mathilde
Fabing, Isabelle
Carayon, Chantal
Silvia Orena, Béatrice
Rosalia Pasca, Maria
Voitenko, Zoia
Lherbet, Christian
Baltas, Michel
Мова основного тексту :
Англійська
eKNUTSHIR URL :
Том :
3
Випуск :
1
ISSN :
2312-3222
Початкова сторінка :
82
Кінцева сторінка :
96
Цитування :
[APA 7] Menendez, C., Mori, G., Maillot, M., Fabing, I., Carayon, C., Silvia Orena, B., Rosalia Pasca, M., Voitenko, Z., Lherbet, C., & Baltas, M. (2015). Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents. French-Ukrainian Journal of Chemistry, 3(1), 82–96. https://doi.org/10.17721/fujcV3I1P82-96
[ДСТУ] Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents / C. Menendez et al. French-Ukrainian Journal of Chemistry. 2015. Vol. 3, no. 1. P. 82—96. DOI: 10.17721/fujcV3I1P82-96 (date of access: 18.07.2026).
A new series of β-hydroxytriazoles were synthesized and evaluated as Mycobacterium tuberculosis inhibitors. Our strategy implied the synthesis of alkyne precursors through a Barbier reaction between benzaldehydes and propargyl bromide followed by click chemistry to afford substituted β-hydroxyl benzyltriazoles. These compounds are also key intermediates either for oxidation reactions leading to α,β-diketotriazoles or for elimination reactions affording styryl triazoles. Evaluation of all new compounds for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv resulted in compounds with MIC up to 7 μM.
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