Antituberculosis Activity of Some 3,6-disubstituted 1,2,4,5-tetrazines

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.