Fragment Based Simplification of Bedaquiline

• In: Short Communications A1 on Monday, 22 May 2017, 13:30-15:00
• At: Stockholm (Sweden) (2017)
• 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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