New ones are being developed synthetic antibiotics superpower able to suppress “superbugs“, included the MRSA, without detectable resistance. To declare it in a recent research were the scientists of theLiverpool University.
Further information on the study can be found at the site of the University of Liverpool.
Synthetic antibiotics: a pioneering study that could save many lives
The team of scientists developed simplified synthetic antibiotic versions of the molecule teixobactin, used by producing bacteria to kill other bacteria in the soil. The researchers created and tested a unique library of synthetic versions of the antibiotic “that changes the rules of the game “, optimizing key characteristics of the drug to improve efficacy and safety, as well as enabling large-scale production at low cost.
Lead researcher Dr. Ishwar Singh he has declared: “The introduction of synthetic diversity to generate the synthetic teixobactin library is important to overcome the high failure rates associated with the later stages of drug development “.
Dr. Singh’s pioneering research is led by an expert in antimicrobial drug discovery and development and medicinal chemistry at the Center of Excellence in Infectious Diseases Research (CEIDR) in Liverpool. The latest results were achieved as part of a Small Business Research Initiative (SBRI) project, funded by the Department of Health and Social Care. This program was implemented by Innovate UK on behalf of DHSC, with the aim of creating five lead compounds for future use in the battle against antimicrobial resistance (AMR).
The research produced evidence on synthetic antibiotics such as Simplified synthetic teixobactins which suppress a wide range of bacteria taken from individuals, where current antibiotics produce no results. Experts also successfully eradicated MRSA in mice and found that it accumulated at infection sites for up to 24 hours in larger quantities than needed to kill superbugs.
These findings are a key clue for the development of future therapies with a single dose of teixobactin per day for life-threatening systemic resistant bacterial infections. Synthetic teixobactins have been found to be more robust and stable at room temperature for years, so they don’t need a cold chain for distribution and storage, so they have the potential to address resistant bacterial infections in diverse clinical settings globally.
Dr. Singh also identified designs and methods for “to increaseCheap synthetic antibiotics based on natural teixobactin, too expensive in the past. By replacing certain amino acids on the molecule with low-cost commercially available alternatives, the cost of materials has been reduced by more than 2,000 times, while improving efficacy and safety. Researchers developed highly efficient solid-phase synthesis using automation, accelerating a single coupling step from 30 hours to just 10 minutes with high yields.
Not only that, the team optimized the preparation to increase the yield from 30mg to 1g and beyond. The process can now be adapted for applications up to 1 kg in scale or larger by simply increasing the scale and size of the reactor. Scalability is an important key to commercial manufacturing to realize the therapeutic potential of synthetic teixobactins.
Dr. Singh stated: “Our motivation is to adapt the natural teixobactin molecule and make it suitable for human use. This is a journey. Through this project we have shown that we can make low-cost, high-safety synthetic molecules that powerfully kill resistant bacteria in mice. The advantage of synthetic diversity is that we can select or deselect properties and modify molecules to affect potency and other drug-like qualities. “
“Our ultimate goal – Continued the scientist – It is to have a number of vital drugs from our modular synthetic teixobactin platform that can be used as a “last line of defense” against superbugs to save lives currently lost to AMR. “
“Our next steps will be to focus on the central benefit of synthetic teixobactin to overcome multi-resistant bacteria in different disease models, augment the process, followed by safety testing, which if successful, could potentially be used in hospitals as a new drug trial. and will be transformed into a drug suitable for the treatment of resistant bacterial infections in humans globally. We will work with CEIDR colleagues who have antimicrobial experience from drug discovery to clinic to develop synthetic teixobactins into vital drugs. “
Professor William Hope, director of CEIDRhe has declared: “New synthetic antibiotics are urgently needed to address unmet medical needs for multiple, highly drug-resistant bacteria. Infections due to these superbugs impair treatment results for many patients. Teixobactins have the potential to provide valuable new treatment options for patients across the UK and around the world. “
The secretary of health and social assistance Sajid Javid he has declared: “It is fantastic to see such groundbreaking work as this happening in the UK, another clear example of this country at the forefront of scientific advances that can benefit people around the world. “.
“The growing tide of antimicrobial resistance is threatening the future of modern medicine, with currently treatable infections becoming incurable and routine medical procedures such as Caesarean sections are becoming much less safe. “
“Continuing to develop new drugs is essential to ensure that this risk does not become a reality and that is why these results are so encouraging. “
Dr. Phil PackerHead of Innovation for AMR and Vaccines at Innovate UK, he has declared: “This has been an excellent project and we sincerely hope that this work will continue and go much further. There is a lot of development going on in the AMR space, as far as it focuses on modifying the classes of existing molecules. This is useful in the short term, but these scaffold molecules are already familiar to bacteria, which makes it more likely that resistance against these molecules will develop. There is a lack in the AMR pipeline for new classes of antibiotics, and this is where this project fits in. “
“We are pleased with the findings, which validated synthetic teixobactin’s promise to address resistant bacterial infections when currently used antibiotics fail. We look forward to following this journey closely in the future“.
A review of the AMR commissioned by the UK government predicted that by 2050 another 10 million people will succumb to drug-resistant infections each year. Furthermore, it is believed that COVID-19 is accelerating the global threat of antimicrobial resistance as many hospitalized infected patients receive antibiotics to control secondary bacterial infections. Increased use of antibiotics leads to increased bacterial resistance. The development of new antibiotics that can be used as a last resort when other drugs are ineffective is therefore a crucial area of study for healthcare researchers around the world.
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