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Updated: May 11, 2026

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
[Antituberculosis properties of methyldioxotetrahydropyrimidine sulfonisonicotinoyl hydrazide]
Abstract:
Antituberculosis properties of methyldioxotetrahydropyrimidine sulfonisonicotinoyl hydrazide (MSH) registered in Russia under the name of tubosan of the class of immunotropic agents were investigated with the use of 78 clinical isolates of Mycobacterium tuberculosis (MBT). In concentration of 60 or 80 mcg/ml the drug showed significant antituberculosis activity. The effect of MSH on drug susceptible MBT was bactericidal. The effect of MSH on the drug resistant MBT (with the isoniazid MIC of 1 mcg/ml) was bactericidal in 75% of the cases and bacteriostatic in 25% of the cases. With the use of MBT resistant to isoniazid in a concentration of 10 mcg/ml the antituberculosis effect was observed in 47% of the cases. The complex treatment of 102 patients with destructive forms of tuberculosis in a daily dose of 800-1200 mg for 2-5 months provided significant clinicoroentgenologic positive dynamics of the process in 75% of the patients. The destructive cavities closed up in 30% of the patients and reduction of the destruction dimentions up to 0.5-2 cm was stated in 45% of the patients. In the control group of 40 patients insignificant dynamics of the destructive processes was observed only in 40% of the patients. Satisfactory tolerability of the drug was registered. The immunity status parameters improved with increase of the total number of T-lymphocytes and phagocytosis indices. The study showed that MSH was efficient in complex therapy of tuberculosis patients allow for increased number of cases with drug resistant tuberculosis.
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