Publication: Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens
Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens
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Matsushita, T., Sati, G. C., Kondasinghe, N., Pirrone, M. G., Kato, T., Waduge, P., Kumar, H. S., Sanchon, A. C., Dobosz-Bartoszek, M., Shcherbakov, D., Juhas, M., Hobbie, S. N., Schrepfer, T., Chow, C. S., Polikanov, Y. S., Schacht, J., Vasella, A., Böttger, E. C., & Crich, D. (2019). Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens. Journal of the American Chemical Society, 141(12), 5051–5061. https://doi.org/10.1021/jacs.9b01693
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Infectious diseases due to multidrug-resistant pathogens, particularly carbapenem-resistant Enterobacteriaceae (CREs), present a major and growing threat to human health and society, providing an urgent need for the development of improved potent antibiotics for their treatment. We describe the design and development of a new class of aminoglycoside antibiotics culminating in the discovery of propylamycin. Propylamycin is a 4'-deoxy-4'-alkyl paromomycin whose alkyl substituent conveys excellent activity against a broad spectrum of ESK
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Creators (Authors)
- Matsushita, Takahiko
- Sati, Girish C
- Kondasinghe, Nuwan
- Pirrone, Michael G
- Kato, Takayuki
- Waduge, Prabuddha
- Kumar, Harshitha Santhosh
- Sanchon, Adrian Cortes
- Dobosz-Bartoszek, Malgorzata
- Shcherbakov, Dimitri
- Juhas, Mario
- Hobbie, Sven N
- Schrepfer, Thomas
- Chow, Christine S
- Polikanov, Yury S
- Schacht, Jochen
- Vasella, Andrea
- Böttger, Erik C
- Crich, David
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Matsushita, T., Sati, G. C., Kondasinghe, N., Pirrone, M. G., Kato, T., Waduge, P., Kumar, H. S., Sanchon, A. C., Dobosz-Bartoszek, M., Shcherbakov, D., Juhas, M., Hobbie, S. N., Schrepfer, T., Chow, C. S., Polikanov, Y. S., Schacht, J., Vasella, A., Böttger, E. C., & Crich, D. (2019). Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens. Journal of the American Chemical Society, 141(12), 5051–5061. https://doi.org/10.1021/jacs.9b01693
