title: Total Synthesis of Teixobactin.
abstract: The first total synthesis of the cyclic depsipeptide natural product teixobactin is described. Synthesis was achieved by solid-phase peptide synthesis, incorporating the unusual l-allo-enduracididine as a suitably protected synthetic cassette and employing a key on-resin esterification and solution-phase macrolactamization. The synthetic natural product was shown to possess potent antibacterial activity against a range of Gram-positive pathogenic bacteria, including a virulent strain of Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus (MRSA).
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Giltrap
authors.forename: Luke J
authors.initials: LJ
authors.lastname: Dowman
authors.forename: Gayathri
authors.initials: G
authors.lastname: Nagalingam
authors.affiliation: Department of Chemistry and Biochemistry, University of California , Santa Cruz, California 95064, United States.
authors.forename: Jessica L
authors.initials: JL
authors.lastname: Ochoa
authors.affiliation: Department of Chemistry and Biochemistry, University of California , Santa Cruz, California 95064, United States.|Department of Chemistry, Simon Fraser University , Burnaby, British Columbia BC V5A 1S6, Canada.
authors.forename: Roger G
authors.initials: RG
authors.lastname: Linington
authors.forename: Warwick J
authors.initials: WJ
authors.lastname: Britton
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Payne
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003500:Cyclization; D047630:Depsipeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D004951:Esterification; D006865:Hydrogenation; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D047630:Depsipeptides; C000594838:teixobactin