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SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs

Leupyrrins are highly potent antifungal agents. A structure–activity‐relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified...

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Detalles Bibliográficos
Autores principales: Wosniok, Paul R., Knopf, Christopher, Dreisigacker, Sandra, Orozco‐Rodriguez, J. Manuel, Hinkelmann, Bettina, Mueller, Peter P., Brönstrup, Mark, Menche, Dirk
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7756798/
https://www.ncbi.nlm.nih.gov/pubmed/32608026
http://dx.doi.org/10.1002/chem.202002622
Descripción
Sumario:Leupyrrins are highly potent antifungal agents. A structure–activity‐relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified leupylogs that incorporate a stable and readily available aromatic side chain. For their synthesis a concise strategy is described that enables a short and versatile access.