119425-84-2Relevant academic research and scientific papers
Structure-Activity Relationship Studies of a Series of Semisynthetic Lipopeptides Leading to the Discovery of Surotomycin, a Novel Cyclic Lipopeptide Being Developed for the Treatment of Clostridium difficile -Associated Diarrhea
Yin, Ning,Li, Jing,He, Yong,Herradura, Prudencio,Pearson, Andre,Mesleh, Michael F.,Mascio, Carmela T.,Howland, Karen,Steenbergen, Judith,Thorne, Grace M.,Citron, Diane,Van Praagh, Andrew D. G.,Mortin, Lawrence I.,Keith, Dennis,Silverman, Jared,Metcalf, Chester
supporting information, p. 5137 - 5142 (2015/07/02)
Novel cyclic lipopeptides with different acyl tails were synthesized via a semisynthetic approach. Structure-activity relationship studies revealed that lipophilicity, chain length, and the location of key aromatic functionalities of the tail modulated activity. The lead compound surotomycin exhibited significantly improved in vitro activity compared with daptomycin (MIC90 0.5 vs 2 μg/mL) against Clostridium difficile including NAP1 epidemic strains. In hamster efficacy studies, surotomycin protected animals at a dose of 0.5 mg/kg, PO.
NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS
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, (2010/08/07)
The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacte
