Combinatorial discovery process yields antimicrobial peptoids

N-alkylated glycine trimers are generically referred to as peptoids. The identification of antimicrobial peptoids from a statistically unbiased diverse combinatorial chemistry library led to the design of the optimization peptoid library that we describe in this manuscript. This optimization library...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1999-09, Vol.7 (9), p.1781-1785
Main Authors: NG, S, GOODSON, B, EHRHARDT, A, MOOS, W. H, SIANI, M, WINTER, J
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Combinatorial Chemistry Techniques
Escherichia coli - drug effects
Escherichia coli - growth & development
Medical sciences
Microbial Sensitivity Tests
Oligopeptides - chemical synthesis
Oligopeptides - chemistry
Oligopeptides - pharmacology
Peptoids
Pharmacology. Drug treatments
Protein Conformation
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
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Description
Summary:N-alkylated glycine trimers are generically referred to as peptoids. The identification of antimicrobial peptoids from a statistically unbiased diverse combinatorial chemistry library led to the design of the optimization peptoid library that we describe in this manuscript. This optimization library was designed using structural information from the most active peptoids in the unbiased library. Screening of the optimization library for antimicrobial activity identified a single pool of peptoids with activity against both Staphylococcus aureus and Escherichia coli. The active peptoids from this pool were active against drug sensitive and drug resistant organisms and represent novel antibacterial compounds.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(99)00132-7