SYNTHESIS AND ANTI-TRICHINELLA SPIRALIS ACTIVITY IN VITRO OF SOME NEW 1H-BENZIMIDAZOLES

Novel derivatives of 1H-benzimidazole which combine into a single molecule two pharmacophores – the benzimidazole and piperazine rings possessing antihelmintic activity have been synthesized. Their structures were confirmed by IR, 1H NMR, 13C NMR and elemental analysis techniques.The compounds exhibited remarkable effect on the viability of isolated Trichinella spiralis muscle larvae in in vitro model at a dose of 100 μg/ml after 24 h. The results obtained by the hepatotoxicity test showed that compound 4 had the lowest hepatotoxity.Novel derivatives of 1H-benzimidazole which combine into a single molecule two pharmacophores – the benzimidazole and piperazine rings possessing antihelmintic activity have been synthesized. Their structures were confirmed by IR, 1H NMR, 13C NMR and elemental analysis techniques.The compounds exhibited remarkable effect on the viability of isolated Trichinella spiralis muscle larvae in in vitro model at a dose of 100 μg/ml after 24 h. The results obtained by the hepatotoxicity test showed that compound 4 had the lowest hepatotoxity

Treatment of hepatic and pulmonary hydatidosis with albendazole and praziquantel

Conservative treatment of human hydatidosis (cystic echinococcosis) with albendazole has improved significantly the prognosis of the disease. But its therapeutic effectiveness is 30 – 70 %. There is some evidence that the effectiveness of albendazole can be enhanced by praziquantel but there is no strict recommendation for the use of praziquantel as part of long-term drug therapy for hydatidosis

New 1H-benzimidazole-2-yl hydrazones with combined antiparasitic and antioxidant activity

Funding Information: This work has been nancially supported by the National Science Fund of Bulgaria, Contract KII-06-H39/4. Research equipment of Distributed Research Infrastructure INFRAMAT, part of Bulgarian National Roadmap for Research Infrastructures, supported by Bulgarian Ministry of Education and Science was used in a part of this investigation. Publisher Copyright: © The Royal Society of Chemistry 2021.Parasitic infections, caused mainly by the speciesTrichinella spiralis(T. spiralis), are widespread around the world and lead to morbidity and mortality in the population. Meanwhile, some studies have showed that these parasites induce oxidative stress in the infected host. With the aim of developing a class of compounds combining anthelmintic with antioxidant properties, a series of new benzimidazolyl-2-hydrazones5a-l, bearing hydroxyl- and methoxy-groups, were synthesized. The anthelmintic activity on encapsulatedT. spiraliswas studiedin vitrothus indicating that all hydrazones were more active than the clinically used anthelmintic drugs albendazole and ivermectin.5band5dkilled the total parasitic larvae (100% effectiveness) after 24 hours incubation period at 37 °C in both concentrations (50 and 100 μg ml−1). The antioxidant activity of the target compounds was elucidatedin vitroagainst stable free radicals DPPH and ABTS as well as iron induced oxidative damage in model systems containing biologically relevant molecules lecithin and deoxyribose. The two 2,3- and 3,4-dihydroxy hydrazones5band5dwere the most effective radical scavengers in all studied systems. DFT calculations were applied to calculate the reaction enthalpies in polar and nonpolar medium and estimate the preferred mechanism of antioxidant activity. The relative radical scavenging ability of compounds5a-lshowed a good correlation to the experimentally observed trends. It was found that the studied compounds are capable to react with various free radicals - ˙OCH3, ˙OOH and ˙OOCH3, through several possible reaction pathways - HAT in nonpolar medium, SPLET in polar medium and RAF in both media.publishersversionpublishe