The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives.
| Autor: | Platonova YB; Department of Chemistry, Lomonosov Moscow State University, 1 Leninskie Gory, Moscow 119991, Russian Federation; Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severny proezd, Chernogolovka, Moscow Region 142432, Russian Federation., Volov AN; Department of Chemistry, Lomonosov Moscow State University, 1 Leninskie Gory, Moscow 119991, Russian Federation. Electronic address: volovalexander@gmail.com., Tomilova LG; Department of Chemistry, Lomonosov Moscow State University, 1 Leninskie Gory, Moscow 119991, Russian Federation; Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severny proezd, Chernogolovka, Moscow Region 142432, Russian Federation. |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Aug 15; Vol. 30 (16), pp. 127351. Date of Electronic Publication: 2020 Jun 13. |
| DOI: | 10.1016/j.bmcl.2020.127351 |
| Abstrakt: | A series of new 5-alkynyl-substituted uracil and uridine derivatives were synthesised via palladium-catalysed Sonogashira cross-coupling reaction of 5-bromo-pyrimidine base with terminal acetylenes with good yields in DMF at room temperature. All obtained compounds were tested for antimycobacterial activity against Mycobacetrium bovis and Mycobacterium tuberculosis (H37Ra) at concentrations of 1-100 µg/ml using MABA test. Obtained results revealed that most of tested uracil derivatives exhibited high antimycobacterial activity (MIC Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2020 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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