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Antituberculosis activity of some 3,6-disubstituted 1,2,4,5-tetrazines

Rashida I. Ishmetova, Ilya N. Ganebnykh, Nina K. Ignatenko, Irina G. Ovchinnikova, Olga V. Fedorova, Sergei N. Skornyakov, Gennady L. Rusinov

Abstract


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.

Keywords


3,6-disubstituted 1,2,4,5-tetrazines; 1,2,4,5-tetrazine podands; antimycobacterial activity; acute toxicity

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References


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DOI: https://doi.org/10.15826/chimtech.2024.11.4.14

Copyright (c) 2024 Rashida I. Ishmetova, Ilya N. Ganebnykh, Nina K. Ignatenko, Irina G. Ovchinnikova, Olga V. Fedorova, Sergei N. Skornyakov, Gennady L. Rusinov

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