Abstract
A series of thiosemicarbazide derivatives was designed and synthesized by reaction of carboxylic acid hydrazide with isothiocyanates. The molecular structures of the investigated thiosemicarbazides were confirmed and characterized by spectroscopic analysis. The conformational preference of carbonylthiosemicarbazide chain and intra- and intermolecular interactions in the crystalline state were characterized using X-ray analysis. The antituberculosis activity of the target compounds were tested in vitro against four Mycobacterium strains: M. H37Ra, M. phlei, M. smegmatis, M. timereck. The most active compounds were those with 2-pyridine ring. They exhibited lower minimal inhibitory concentration (MIC) values in the range 7.81–31.25 μg/mL in comparison to the other isomers. Compound 5 had activity against M. smegmatis at a concentration of 7.81 μg/mL whereas compound 2 had activity against all tested strains at a concentration of 15.625 μg/mL. The molecular docking studies were performed for investigated compounds using the Mycobacterium tuberculosis glutamine synthetase MtGS as their molecular target.
Highlights
Tuberculosis is the one of the most common infectious diseases worldwide [1]
In our work we propose the synthesis of Isoniazide analogs as compounds with potential antitubercular activity
The methods of synthesis of thiosemicarbazide derivatives are known and described in the literature [27,28,29] they require continuous modifications depending on the substrates used
Summary
Tuberculosis is the one of the most common infectious diseases worldwide [1]. To AIDS (Acquired Immune Deficiency Syndrome), it is the leading cause of death in the world. Despite the availability of tuberculosis treatment, about 9 million new cases of tuberculosis are reported each year, and 1.5 million cases are fatal. The worst epidemiological situation is in Third World countries, where the incidence rates range from 100–300 cases per 100,000 inhabitants [2]. 95% of cases fall to the developing countries of Asia, Africa, Brazil and Russia. The results of treatment are still not satisfactory. The success rate for new cases and surgeries reported in 2013 was
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