title: A positional scanning combinatorial library of peptoids as a source of biological active molecules: identification of antimicrobials.
abstract: A positional scanning library of N-alkylglycine trimers (peptoids) containing over 10 000 compounds has been synthesized on solid phase. The synthetic pathway involved the use of the submonomer strategy and a set of 22 commercially available primary amines as a chemical diversity source. The unbiased nature of the library allowed its screening against a variety of biological targets, leading to the identification of individual peptoids exhibiting remarkable biological activities (García-Martínez, C. et al. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 2374. Montoliu, et al. J. Pharm. Exp. Therap. 2002, 302, 29. Planells-Cases, R., et al. J. Pharm. Exp. Therap. 2002, 302, 163). In the present work, the screening of this library against a panel of Gram-positive and Gram-negative bacteria led to the identification of different compounds exhibiting antimicrobial activity.
authors.affiliation: Department of Biological Organic Chemistry, I.I.Q.A.B. (C.S.I.C.), E-08034 Barcelona, Spain.
authors.forename: Marc
authors.initials: M
authors.lastname: Humet
authors.forename: Teresa
authors.initials: T
authors.lastname: Carbonell
authors.forename: Isabel
authors.initials: I
authors.lastname: Masip
authors.forename: Francisco
authors.initials: F
authors.lastname: Sánchez-Baeza
authors.forename: Puig
authors.initials: P
authors.lastname: Mora
authors.forename: Emilia
authors.initials: E
authors.lastname: Cantón
authors.forename: Miguel
authors.initials: M
authors.lastname: Gobernado
authors.forename: Concepción
authors.initials: C
authors.lastname: Abad
authors.forename: Enrique
authors.initials: E
authors.lastname: Pérez-Payá
authors.forename: Angel
authors.initials: A
authors.lastname: Messeguer
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D008826:Microbial Sensitivity Tests; D019151:Peptide Library; D034444:Peptoids / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D019151:Peptide Library; D034444:Peptoids