Antituberculosis activity of some 3,6-disubstituted 1,2,4,5-tetrazines
The increase in the incidence of tuberculosis, especially in the post-Covid period, associated with the presence of latent infections and multiple drug resistance, dictates the need to develop new antimicrobial drugs. Here we wish to report the synthesis of 3,6-disubstituted 1,2,4,5-tetrazine derivatives containing N-, O- and C-nucleophile residues, as well as pharmacophoric hydrazone and oligooxyethylene fragments, and their screening against the pathogen Mycobacterium tuberculosis. Substances with pronounced antimycobacterial activity in vitro were identified (MIC = 0.18–3.12 μg/ml). An acute toxicity in vivo and membranotropic properties towards biometals have been studied for the most active compounds.
Authors
- I.N. Ganebnykh (ORCID: https://orcid.org/0000-0002-8487-8448)
- Olga V. Fedorova (ORCID: https://orcid.org/0000-0001-9355-283X)
- Р.И. Ишметова
- Gennady L. Rusinov (ORCID: https://orcid.org/0000-0001-8567-9435)
- N.K. Ignatenko (ORCID: https://orcid.org/0000-0003-2362-4556)
- Sergey Skornyakov (ORCID: https://orcid.org/0000-0002-9942-3008)
- I.G. Ovchinnikova (ORCID: https://orcid.org/0000-0002-3304-6553)
Institutions
- Ural Federal University (RU)
- Institute of Organic Synthesis (RU)
- Ural research Institute of Phthisiopulmonology (RU)
Publication Details
- Journal
- Chimica Techno Acta
- Published
- 2024-11-20
- DOI
- https://doi.org/10.15826/chimtech.2024.11.4.14
- Citations
- 3
- Primary Topic
- Synthesis and Characterization of Heterocyclic Compounds
- Type
- article
- Field-Weighted Citation Impact
- 0.75
Funders
- Ural Branch, Russian Academy of Sciences
- Ministry of Science and Higher Education of the Russian Federation
- Russian Academy of Sciences
- Postovsky Institute of Organic Synthesis