Publication: Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation
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Dorst, A., Berg, R., Gertzen, C. G. W., Schäfle, D., Zerbe, K., Gwerder, M., Schnell, S. D., Sander, P., Gohlke, H., & Gademann, K. (2020). Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation. ACS Medicinal Chemistry Letters, 11(12), 2414–2420. https://doi.org/10.1021/acsmedchemlett.0c00381
Abstract
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Abstract
The glycoslated macrocyclic antibiotic fidaxomicin (1, tiacumicin B, lipiarmycin A3) displays good to excellent activity against Gram-positive bacteria and was approved for the treatment of Clostridium difficile infections (CDI). Among the main limitations for this compound, its low water solubility impacts further clinical uses. We report on the synthesis of new fidaxomicin derivatives based on structural design and utilizing an operationally simple one-step protecting group-free preparative approach from the natural product. An incr
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- Dorst, Andrea
- Berg, Regina
- Gertzen, Christoph G W
- Schäfle, Daniel
- Zerbe, Katja
- Gwerder, Myriam
- Schnell, Simon D
- Sander, Peter
- Gohlke, Holger
- Gademann, Karl
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Dorst, A., Berg, R., Gertzen, C. G. W., Schäfle, D., Zerbe, K., Gwerder, M., Schnell, S. D., Sander, P., Gohlke, H., & Gademann, K. (2020). Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation. ACS Medicinal Chemistry Letters, 11(12), 2414–2420. https://doi.org/10.1021/acsmedchemlett.0c00381
