چكيده به لاتين
Today, the relentless expansion of microbial resistance to antibiotics on the market has become a major concern in public health. In the pursuit of new antimicrobial compounds, two drugs, Nitrofurantoin and Nifurtimox, have been considered. Nitrofurantoin is used to treat urinary tract infections. The nitrofurantoin inside the bacterial cell is reduced by flavoproteins (reductase) and damages ribosomal proteins by forming highly active intermediates. Activation of this drug in bacterial cells is much faster than in human cells. It is important to note that the mechanism of action of the complex has slowed its resistance. On the other hand, the anti-parasit drug Nifurtimox, which is used in the treatment of American Trypanosomiasis, is converted to a metabolic nitro radical anion which results in the breakdown of DNA. It also regenerates under enzymatic reactions and converts to active oxygen radicals, such as superoxides, which accumulate in the parasite and lead to the death of the parasite. Both drugs contain 5-nitro heteroaryl methylidene hydrazine. In this study, design and synthesis of new derivatives by the integration of active heteroaromatic rings in 5-nitro heteroaryl methylidene hydrazine is inspired by the mentioned drugs and their antimicrobial effect is evaluated in vitro. It was observed that by applying these changes to the above compounds, we obtained new, safe and effective compounds on microbial strains and helped to overcome the drug resistance problem.
