Abstract
Parasitic infections caused by different species of intestinal helminths still poses a threat to public health. There is a need to search for new, effective anthelmintic drugs. A series of novel thiosemicarbazides were synthesized and evaluated for their in vitro anthelmintic activity. The preliminary results showed that the most of synthesized compounds were very active. 4-Phenyl-1-[(1-methyl-4-nitroimidazol-2-yl)carbonyl]thiosemicarbazide and 4-(3-chlorophenyl)-1-[(1-methyl-4-nitroimidazol-2-yl)carbonyl]thiosemicarbazide showed a 100% mortality of nematodes and a high anthelmintic activity in both tested concentrations.
Highlights
Nothing could be further from the truth than that nowadays the problem of parasitic diseases caused by different species of intestinal helminths is no longer valid
Substituents for synthesis were selected in such a way that on the basis of the results of the biological studies, it was possible to determine the effect of the type of substituent on the anthelmintic activity
Based on the results obtained, it can be concluded that the presence of a halogen in the phenyl ring of thiosemicarbazide derivatives determines the activity
Summary
Nothing could be further from the truth than that nowadays the problem of parasitic diseases caused by different species of intestinal helminths is no longer valid. One of the class of simple compounds that were evaluated for parasiticidal activity are thiosemicarbazones. These molecules were active against Plasmodium falcipilarum, Trypanosoma equipedum, Trypanosoam crusi, Trypanosoma brucei, and Toxoplasma gondii [6,7,8,9]. We obtained earlier and evaluated some thiosemicarbazides with good activity towards T. gondii [21,22]. Continuing in this direction, we designed and obtained thiosemicarbazide derivatives having a nitroimidazole substituent found in Metronidazole—the popular available antiparasitic drug
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