Proceedings of the National Academy of Sciences · 2020 · 61 citations · 25 references
PharmacyMedicinal ChemistryPharmacologyAntimicrobial ResistanceDrug DesignDrug DiscoveryAntibacterial PharmacologyAntibiotic ResistanceLead Compound DesignLead DiscoveryAntibiotic DiscoveryBroad-spectrum AntibioticsDrug-resistant PathogensMultidrug-resistant PathogensMurine ModelsNovel Antibacterial AgentsNovel Antibacterial Drug DiscoveryPan-drug Resistance
PIM1-resistant mutants did not emerge. Although PIM1 was efficacious as a topical agent, intraperitoneal administration of PIM1 in mice showed some toxicity. We synthesized a PIM1 derivative, PIM1D, which is less hydrophobic than PIM1. PIM1D did not show evidence of toxicity but retained antibacterial activity and showed efficacy in murine sepsis infections. Our evidence indicates the PIMs have potential as candidates for development of new drugs for treatment of pan-resistant bacterial infections.
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Anna-Pelagia Magiorakos, Arjun Srinivasan, Roberta B. Carey et al. · Clinical Microbiology and Infection · 2011 · 14K citations
A new antibiotic kills pathogens without detectable resistance
Losee L. Ling, Tanja Schneider, Aaron J. Peoples et al. · Nature · 2015 · 2.4K citations · Full text
Samuel M. Moskowitz, Robert K. Ernst, Samuel I. Miller · Journal of Bacteriology · 2003 · 414 citations · Full text