A positional scanning combinatorial library of peptoids as a source of biological active molecules: identification of antimicrobials.
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.
Humet
Marc
M
Department of Biological Organic Chemistry, I.I.Q.A.B. (C.S.I.C.), E-08034 Barcelona, Spain.
Carbonell
Teresa
T
Masip
Isabel
I
Sánchez-Baeza
Francisco
F
Mora
Puig
P
Cantón
Emilia
E
Gobernado
Miguel
M
Abad
Concepción
C
Pérez-Payá
Enrique
E
Messeguer
Angel
A
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*
D000900:Anti-Bacterial Agents; D019151:Peptide Library; D034444:Peptoids