title: Flexible synthesis and evaluation of diverse anti-Apicomplexa cyclic peptides.
abstract: A modular approach to synthesize anti-Apicomplexa parasite inhibitors was developed that takes advantage of a pluripotent cyclic tetrapeptide scaffold capable of adjusting appendage and skeletal diversities in only a few steps (one to three steps). The diversification processes make use of selective radical coupling reactions and involve a new example of a reductive carbon-nitrogen cleavage reaction with SmI2. The resulting bioactive cyclic peptides have revealed new insights into structural factors that govern selectivity between Apicomplexa parasites such as Toxoplasma and Plasmodium and human cells.
authors.affiliation: Département de Pharmacochimie Moléculaire, Université Joseph Fourier-Grenoble 1, CNRS UMR 5063, CNRS ICMG FR 2607, bâtiment André Rassat, 470 rue de la Chimie, F-38041 Grenoble Cedex 9, France.
authors.forename: Mariam
authors.initials: M
authors.lastname: Traoré
authors.forename: Flore
authors.initials: F
authors.lastname: Mietton
authors.forename: Danièle
authors.initials: D
authors.lastname: Maubon
authors.forename: Marine
authors.initials: M
authors.lastname: Peuchmaur
authors.forename: Flaviane Francisco
authors.initials: FF
authors.lastname: Hilário
authors.forename: Rossimiriam
authors.initials: R
authors.lastname: Pereira de Freitas
authors.forename: Alexandre
authors.initials: A
authors.lastname: Bougdour
authors.forename: Aurélie
authors.initials: A
authors.lastname: Curt
authors.forename: Marjorie
authors.initials: M
authors.lastname: Maynadier
authors.forename: Henri
authors.initials: H
authors.lastname: Vial
authors.forename: Hervé
authors.initials: H
authors.lastname: Pelloux
authors.forename: Mohamed-Ali
authors.initials: MA
authors.lastname: Hakimi
authors.forename: Yung-Sing
authors.initials: YS
authors.lastname: Wong
mesh_terms: D016782:Apicomplexa / Q000737:chemistry*; D006790:Host-Parasite Interactions; D006801:Humans; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry; D010961:Plasmodium / Q000737:chemistry*; D014122:Toxoplasma / Q000737:chemistry*
chemical_list: D010456:Peptides, Cyclic