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
Mini-Reviews in Medicinal Chemistry
Title: Mutilins Derivatives: From Veterinary to Human-used Antibiotics
Volume: 9 Issue: 12
Author(s): Changhua Hu and Yi Zou
Affiliation:
Keywords: Antibacterial, pleuromutilin, tiamulin, valnemulin, retapamulin, structure-activity relationship (SAR), purine ring, piperazine ring spacer, water-soluble, metabolic stability
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.
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Cite this article as:
Hu Changhua and Zou Yi, Mutilins Derivatives: From Veterinary to Human-used Antibiotics, Mini-Reviews in Medicinal Chemistry 2009; 9 (12) . https://dx.doi.org/10.2174/138955709789957387
DOI https://dx.doi.org/10.2174/138955709789957387 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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