The design and optimisation of the second-generation antibacterial oral streptogramin is reported in terms of semi-synthesis, structure-activity relationships, pharmaco-kinetics properties and antibacterial activities. Our endeavours led to the selection of two new combinations RPR131166/RPR132493 (30/70) and RPR202868/RPR132552 (30/70) whose antibacterial properties will be reported in detail. The overall profile of the latter association, which is currently undergoing clinical development, suggests that it could be useful for the treatment of community-acquired infections.
Keywords: antibacterial, streptogramins, pristinamycins, synergy, ribosome, structure-activity relationships, semi-synthesis
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