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Mini-Reviews in Medicinal Chemistry
ISSN (Print): 1389-5575
ISSN (Online): 1875-5607
VOLUME: 9
ISSUE: 12
DOI: 10.2174/138955709789957387      Price:  $58









Mutilins Derivatives: From Veterinary to Human-used Antibiotics

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Author(s): Changhua Hu and Yi Zou
Pages 1397-1406 (10)
Abstract:
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
Affiliation:
Institute of Modern Biopharmaceuticals, School of Pharmaceutical Sciences, Southwest University, Chongqing 400716, P.R. China.