Mutilins derivatives, which were successfully developed in veterinary medicines such as tiamulin and valnemulin, have regained interest as promising antibacterial agents with potential for human use in the past few years. In 2007, Retapamulin, as the first in a new class of topical antibacterial in the nearly two decades, was approved for use in human skin infections. This review provides a developed process of mutilins derivatives from veterinary to human-used antibiotics and emphasizes the structure activity relationship (SAR) and antibacterial mechanism of mutilins derivatives. Moreover, the semi-synthetic strategy of water-soluble mutilins derivatives and related novel derivatives during 2006-2008 will also be reviewed.
Keywords: Antibacterial, pleuromutilin, tiamulin, valnemulin, retapamulin, structure-activity relationship (SAR), purine ring, piperazine ring spacer, water-soluble, metabolic stability
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