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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Veröffentlicht in:	Journal of medicinal chemistry Jg. 57; H. 4; S. 1428 - 1436
Hauptverfasser:	Ghosh, Chandradhish, Manjunath, Goutham B., Akkapeddi, Padma, Yarlagadda, Venkateswarlu, Hoque, Jiaul, Uppu, Divakara S. S. M., Konai, Mohini M., Haldar, Jayanta
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 27.02.2014
Schlagworte:	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
ISSN:	0022-2623, 1520-4804, 1520-4804
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Zusammenfassung:	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.
Bibliographie:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804 1520-4804
DOI:	10.1021/jm401680a