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Design and synthesis of new vancomycin derivatives
Affiliation:1. College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China;2. Acesys PharmaTech, Inc., Science and Technology Building 24B, 5 Xing Mo Fang Road, Nanjing 210009, China;1. Faculty of Sciences of Monastir, Tunisia;2. Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, USA;1. Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK;2. Novartis Pharma AG, Novartis Institutes for BioMedical Research, Postfach, CH-4002 Basel, Switzerland;1. Institute of Neurobiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria;2. Department of Organic Chemistry, University of Chemical Technologies and Metallurgy, Sofia, Bulgaria;3. Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS-Université Montpellier 1 et Université Montpellier 2, France;1. Department of Life Systems, Sookmyung Women’s University, Seoul 140-742, Republic of Korea;2. Department of Environmental Health Science, Konkuk University, Hwayang-dong 1, Kwangjin-gu, Seoul 143-701, Republic of Korea
Abstract:A set of vancomycin derivatives with lipid chain attached via a glyceric acid linker was designed and synthesized. A concise synthesis towards these derivatives was developed and the IC50s of these new lipoglycopeptides were tested. Some of them showed very potent activity against both vancomycin sensitive and resistant strains.
Keywords:Anti-bacterial  Vancomycin  Synthesis
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