title: New synthetic approaches towards analogues of bedaquiline.
abstract: Multi-drug resistant tuberculosis (MDR-TB) is of growing global concern and threatens to undermine increasing efforts to control the worldwide spread of tuberculosis (TB). Bedaquiline has recently emerged as a new drug developed to specifically treat MDR-TB. Despite being highly effective as a result of its unique mode of action, bedaquiline has been associated with significant toxicities and as such, safety concerns are limiting its clinical use. In order to access pharmaceutical agents that exhibit an improved safety profile for the treatment of MDR-TB, new synthetic pathways to facilitate the preparation of bedaquiline and analogues thereof have been discovered.
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia. Jonathan.baell@monash.edu.
authors.forename: Daniel L
authors.initials: DL
authors.lastname: Priebbenow
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia. Jonathan.baell@monash.edu.
authors.forename: Lisa
authors.initials: L
authors.lastname: Barbaro
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia. Jonathan.baell@monash.edu.
authors.forename: Jonathan B
authors.initials: JB
authors.lastname: Baell
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D001897:Boronic Acids / Q000737:chemistry; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D064687:Diarylquinolines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D018432:Drug Resistance, Multiple / Q000187:drug effects; D012449:Safety
chemical_list: D000900:Anti-Bacterial Agents; D001897:Boronic Acids; D064687:Diarylquinolines; C493870:bedaquiline