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These bisbensimidazole derivatives are a new family of modified small molecules that are highly selective and effective in preventing bacterial resistance. The market for antibacterial drugs stood at $43.9 billion in 2014, representing a large market for both animals and humans. New approaches for the discovery of antibacterial drugs and antibacterial coatings are important in the fight against bacterial resistance. Bacterial DNA topoisomerases are one class of enzymes that help in regulating DNA topology and are very good targets for the development of anticancer or antibacterial agents. Clemson University researchers have developed a new family of modified small molecules that include bisbenzimidazole derivatives as antimicrobials and topoisomerase inhibitors. These modified compounds offer several advantages over existing topoisomerase inhibitors, such as being highly selective and effective in preventing antibacterial activity. These compounds therefore are excellent candidates for clinically relevant antibacterial agents.
Antibacterial coatings; pharmaceuticals; antibiotics
Overall, the results show that bisbenzimidazoles are excellent inhibitors of E. coli DNA topoisomerase I and also display good antibacterial activity. Additionally, and more importantly, the E. coli topoisomerase I inhibition is extremely selective as DNA gyrase and mammalian topoisomerases are not inhibited. Clemson University research findings suggest that the ternary complex formed by the bacterial topoisomerase I has distinct sites for small molecule recognition, as compared to those found in DNA gyrase and mammalian topoisomerases, and these differences could be further exploited for antibacterial drug development. Further studies to investigate the mechanism of antibacterial activity and enzyme inhibition are being investigated and will be reported in due course.
• Utilizes new compounds that take longer to develop bacterial resistance, offering relevant clinical
• Meets market demand for new agents, improving patient care and accessibility to needed antibacterial drugs
Dev Arya, Nihar Ranjan, Fenfei Leng
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