Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents

Autor:	Christophe Menendez, Mathilde Maillot, Maria Rosalia Pasca, Giorgia Mori, Beatrice Silvia Orena, Chantal Carayon, Christian Lherbet, Zoia Voitenko, Isabelle Fabing, Michel Baltas
Rok vydání:	2015
Předmět:	Barbier reaction chemistry.chemical_classification biology Alkyne biology.organism_classification Combinatorial chemistry Redox Mycobacterium tuberculosis chemistry.chemical_compound Elimination reaction chemistry Mycobacterium tuberculosis H37Rv Click chemistry Organic chemistry Propargyl bromide
Zdroj:	French-Ukrainian Journal of Chemistry. 3:82-96
ISSN:	2312-3222
DOI:	10.17721/fujcv3i1p82-96
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::af56e287c3594188aea2193d26e948d8 https://doi.org/10.17721/fujcv3i1p82-96 Zobrazit plný text záznamu