retapamulin has been researched along with valnemulin* in 4 studies
3 review(s) available for retapamulin and valnemulin
| Article | Year |
|---|---|
Efficient antibacterial agents: a review of the synthesis, biological evaluation and mechanism of pleuromutilin derivatives.
Pleuromutilins were discovered as natural-product antibiotics in 1950. The modifications of pleuromutilin lead to the successful development of veterinary medicines such as tiamulin and valnemulin. Retapamulin became the first pleuromutilin approved for use in human skin infections. Recent advances have led to the synthesis of pleuromutilins that combine potent antibacterial activity with favorable pharmaceutical properties, and three new pleuromutilins, BC-3781, BC-3205 and BC-7013, have entered clinical trials. In this review, the key pleuromutilin derivatives, as well as related novel derivatives during 2009-2013, and its antibacterial activities, are presented. Moreover, the antibacterial and resistance mechanism are discussed. Topics: Animals; Anti-Bacterial Agents; Bridged Bicyclo Compounds, Heterocyclic; Diterpenes; Drug Resistance, Bacterial; Humans; Molecular Structure; Pleuromutilins; Polycyclic Compounds; Thioglycolates | 2013 |
Pleuromutilin and its derivatives-the lead compounds for novel antibiotics.
Due to the rapid onset of resistance to most antibacterial drugs, research efforts are focusing on new classes of antibacterials with different mechanisms of action from clinically used antibacterials. Pleuromutilin derivatives have received more and more scientific attention for their unique mechanism of action. Two pleuromutilin derivatives, tiamulin and valnemulin have been successfully developed as antibiotics for veterinary use. Retapamulin, another pleuromutilin derivative has been approved for use in humans in April 2007 by Food and Drug Administration (FDA). It has been shown that there is rarely cross-resistance between pleuromutilin derivatives and other antimicrobial agents, and the development of resistance bacterial is still low. This review will demonstrate mechanism of action of pleuromutilin derivatives and reveal the structure-activity relationship (SAR) of pleuromutilin derivatives. Additionally, the pleuromutilin antibacterial derivative agents in the market, such as tiamulin, valnemulin and retapamulin, will be discussed. It is proposed that new antibacterial agents might be developed from pleuromutilin derivatives in the future. Topics: Animals; Anti-Bacterial Agents; Bridged Bicyclo Compounds, Heterocyclic; Diterpenes; Drug Resistance, Microbial; Humans; Pleuromutilins; Polycyclic Compounds; Structure-Activity Relationship | 2012 |
Mutilins derivatives: from veterinary to human-used antibiotics.
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. Topics: Animals; Anti-Bacterial Agents; Bridged Bicyclo Compounds, Heterocyclic; Diterpenes; Humans; Ketones; Pleuromutilins; Polycyclic Compounds; Structure-Activity Relationship | 2009 |
1 other study(ies) available for retapamulin and valnemulin