title: Synthesis and Biological Evaluation of a Teixobactin Analogue.
abstract: The first synthesis and biological activity of a teixobactin analogue is reported. Substitution of the unusual L-allo-enduracididine residue by the naturally occurring L-arginine was achieved, and the analogue gave an activity trend similar to that of teixobactin (against Gram-postive bacteria) and meropenem, which was approved by the FDA in 1996. The synthetic route used allows for the synthesis of the natural product as well as the development of a program of medicinal chemistry.
authors.forename: Yahya E
authors.initials: YE
authors.lastname: Jad
authors.affiliation: Institute for Research in Biomedicine-Barcelona ,08028 Barcelona, Spain.|CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine , Barcelona Science Park, 08028 Barcelona, Spain.
authors.forename: Gerardo A
authors.initials: GA
authors.lastname: Acosta
authors.forename: Tricia
authors.initials: T
authors.lastname: Naicker
authors.forename: Melissa
authors.initials: M
authors.lastname: Ramtahal
authors.affiliation: Department of Chemistry, Faculty of Science, Alexandria University P.O. Box 426, Ibrahimia, Alexandria 21321, Egypt.|Department of Chemistry, College of Science, King Saud University P.O. Box 2455,Riyadh 11451, Saudi Arabia.
authors.forename: Ayman
authors.initials: A
authors.lastname: El-Faham
authors.forename: Thavendran
authors.initials: T
authors.lastname: Govender
authors.forename: Hendrik G
authors.initials: HG
authors.lastname: Kruger
authors.forename: Beatriz G
authors.initials: BG
authors.lastname: de la Torre
authors.affiliation: Institute for Research in Biomedicine-Barcelona ,08028 Barcelona, Spain.|CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine , Barcelona Science Park, 08028 Barcelona, Spain.|Department of Chemistry, College of Science, King Saud University P.O. Box 2455,Riyadh 11451, Saudi Arabia.|Department of Organic Chemistry, University of Barcelona , 08028-Barcelona, Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
mesh_terms: D001120:Arginine / Q000737:chemistry; D001688:Biological Products / Q000737:chemistry; D047630:Depsipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077731:Meropenem; D015394:Molecular Structure; D013237:Stereoisomerism; D013845:Thienamycins / Q000494:pharmacology
chemical_list: D001688:Biological Products; D047630:Depsipeptides; D013845:Thienamycins; D001120:Arginine; D000077731:Meropenem; C000594838:teixobactin