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Fragment Based Simplification of Bedaquiline

  • At: 2017 FIP Congress in Stockholm (Sweden)
  • Type: Presentation
  • By: CUI, Huaqing (Institute of Materia Medica, Chinese Academy of Medical Sciences, Medicinal Chemistry, Beijing, China)
  • Co-author(s): Huaqing Cui: Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
    Chunxian He: Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
    Laura Preiss: Department of Structural Biology, Max Planck Institute of Biophysics, Frankfurt am Main, Germany
    Bin Wang: Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing, China
    Lei Fu: Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing, China
    Hui Wen: Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
    Xiang Zhang: Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
    Thomas Meier: Department of Life Sciences, Imperial College London, London, United Kingdom
    Dali Yin: Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
  • Abstract:

    Backgrounds

    Bedaquiline is a Food and Drug Administration-approved second-line anti-tuberculosis drug with certain clinical safety concerns. In addition, the synthesis yield of bedaquiline is rather low due to the existence of two adjacent chiral carbons in its structures. Further optimization of bedaquiline to circumvent these problems is

    ..

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Last update 4 October 2019

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