The in vitro activity of thioridazine derivatives against Mycobacterium tuberculosis H37Rv

Written by Schelz Zsuzsanna, Marta Martins, Leonard Amaral, Hajós György, Molnár József

Bacterial resistance against antibiotics is one of the major problems of antibacterial therapy. In Mycobacterium tuberculosis infections, resistance of the causative agent may develop against the drugs of the conventional therapy, such as isoniazid, rifampin, ethambutol, streptomycin and pyrazinamide. In vitro experiments revealed that several phenothiazine derivatives possess antibacterial activity against the antibiotic sensitive and resistant strains of M. tuberculosis. Their application as antitubercular drugs is not indicated due to their side effects. Thioridazine was the most promising phenothiazine because this neuroleptic drug has milder side effects and it is concentrated by macrophages, where the drug is able to kill intracellular Mycobacteria. Twenty-two thioridazine derivatives were involved in our studies in order to determine their antimicrobial activity by the BACTECTM 460-TB radiometric proportion method on M. tuberculosis H37Rv. Results showed that the tested compounds were less active than their parent compound, thioridazine.


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