title: Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
abstract: Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA) have emerged as a global health concern. A new class of compounds featuring an aryl isonitrile moiety has been discovered that exhibits potent inhibitory activity against several clinically-relevant MRSA and VRSA isolates. Structure-activity relationship studies have been conducted to identify the aryl isonitrile group as the key functional group responsible for the observed antibacterial activity. The most potent antibacterial aryl isonitrile analogs (MIC 2 μM) did not show any toxicity against mammalian cells up to a concentration of 64 μM.
authors.affiliation: Department of Chemistry and Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States.
authors.forename: Dexter C
authors.initials: DC
authors.lastname: Davis
authors.affiliation: Department of Comparative Pathobiology, Purdue University College of Veterinary Medicine, West Lafayette, IN 47907, United States.
authors.forename: Haroon
authors.initials: H
authors.lastname: Mohammad
authors.affiliation: Department of Chemistry and Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States.
authors.forename: Kwaku
authors.initials: K
authors.lastname: Kyei-Baffour
authors.affiliation: Department of Comparative Pathobiology, Purdue University College of Veterinary Medicine, West Lafayette, IN 47907, United States.
authors.forename: Waleed
authors.initials: W
authors.lastname: Younis
authors.affiliation: Department of Chemistry and Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States.
authors.forename: Cassidy Noel
authors.initials: CN
authors.lastname: Creemer
authors.affiliation: Department of Comparative Pathobiology, Purdue University College of Veterinary Medicine, West Lafayette, IN 47907, United States. Electronic address: mseleem@purdue.edu.
authors.forename: Mohamed N
authors.initials: MN
authors.lastname: Seleem
authors.affiliation: Department of Chemistry and Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States. Electronic address: mjdai@purdue.edu.
authors.forename: Mingji
authors.initials: M
authors.lastname: Dai
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018938:Caco-2 Cells; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006801:Humans; D016106:Methicillin Resistance / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D020713:Vancomycin Resistance / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D009570:Nitriles
keywords: Antibiotic; Drug resistance; Isonitrile; MRSA; VRSA