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 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.
Chemical Biology and Medicinal Chemistry Laboratory, New Chemistry Unit, Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) , Jakkur, Bengaluru 5600064, Karnataka, India.
Chandradhish
C
Ghosh
Goutham B
GB
Manjunath
Padma
P
Akkapeddi
Venkateswarlu
V
Yarlagadda
Jiaul
J
Hoque
Divakara S S M
DS
Uppu
Mohini M
MM
Konai
Jayanta
J
Haldar
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D004352:Drug Resistance, Microbial; D016984:Enterococcus faecium / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D008856:Microscopy, Fluorescence; D018716:Molecular Mimicry; D034444:Peptoids / Q000737:chemistry / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet
D000900:Anti-Bacterial Agents; D034444:Peptoids