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Biomolecules, Volume 14, Issue 5
May 2024 - 97 articles
Cover Story: There is a constant need to develop new antibiotics to fight resistant bacteria. The synthesis of murepavadin, a cyclic antibacterial peptide in clinical development, was undertaken in order to optimize the preparative protocol, in particular, the use of new activation reagents. Classical approaches using carbodiimide/HOBt rendered low yields. The use of novel reagents based on OxymaPure® and Oxy-B is discussed together with the proper use of chromatographic conditions. Higher yields and purities were obtained. Finally, the antimicrobial activity was tested in Pseudomonas aeruginosa, including highly resistant strains. All murepavadin batches yielded the same highly active MIC values and proved that the chiral integrity of the molecule was preserved in the different synthetic protocols. View this paper
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Biomolecules - ISSN 2218-273X