Small Molecular Antibacterial Peptoid Mimics: The Simpler the Better

The emergence of multidrug resistant bacteria compounded by the depleting arsenal of antibiotics has accelerated efforts toward development of antibiotics with novel mechanisms of action. In this report, we present a series of small molecular antibacterial peptoid mimics which exhibit high in vitro...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 57; no. 4; pp. 1428 - 1436
Main Authors Ghosh, Chandradhish, Manjunath, Goutham B, Akkapeddi, Padma, Yarlagadda, Venkateswarlu, Hoque, Jiaul, Uppu, Divakara S. S. M, Konai, Mohini M, Haldar, Jayanta
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 27.02.2014
Amer Chemical Soc
Subjects
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Chemistry, Medicinal
Chromatography, High Pressure Liquid
Drug Resistance, Microbial
Enterococcus faecium - drug effects
Hemolysis - drug effects
Life Sciences & Biomedicine
Magnetic Resonance Spectroscopy
Mass Spectrometry
Methicillin-Resistant Staphylococcus aureus - drug effects
Microbial Sensitivity Tests
Microscopy, Electron, Scanning
Microscopy, Fluorescence
Molecular Mimicry
Peptoids - chemistry
Peptoids - pharmacology
Pharmacology & Pharmacy
Science & Technology
Spectrophotometry, Ultraviolet
HOST-DEFENSE PEPTIDES
POLYMERS
HELICAL ANTIMICROBIAL PEPTIDES
BACTERIA
PEPTIDOMIMETICS
DE-NOVO DESIGN
SYNTHETIC MIMICS
AMPHIPHILICITY
DERIVATIVES
INFECTIOUS-DISEASES SOCIETY
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Summary:The emergence of multidrug resistant bacteria compounded by the depleting arsenal of antibiotics has accelerated efforts toward development of antibiotics with novel mechanisms of action. In this report, we present a series of small molecular antibacterial peptoid mimics which exhibit high in vitro potency against a variety of Gram-positive and Gram-negative bacteria, including drug-resistant species such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium. The highlight of these compounds is their superior activity against the major nosocomial pathogen Pseudomonas aeruginosa. Nontoxic toward mammalian cells, these rapidly bactericidal compounds primarily act by permeabilization and depolarization of bacterial membrane. Synthetically simple and selectively antibacterial, these compounds can be developed into a newer class of therapeutic agents against multidrug resistant bacterial species.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm401680a