title: Small molecule mimics of DFTamP1, a database designed anti-Staphylococcal peptide.
abstract: Antimicrobial peptides (AMPs) are important templates for developing new antimicrobial agents. Previously, we developed a database filtering technology that enabled us to design a potent anti-Staphylococcal peptide DFTamP1. Using this same design approach, we now report the discovery of a new class of bis-indole diimidazolines as AMP small molecule mimics. The best compound killed multiple S. aureus clinical strains in both planktonic and biofilm forms. The compound appeared to target bacterial membranes with antimicrobial activity and membrane permeation ability similar to daptomycin.
authors.affiliation: College of Pharmacy, University of Nebraska Medical Center, 986125 Nebraska Medical Center, Omaha, NE 68198-6125, United States. Electronic address: ydong@unmc.edu.
authors.forename: Yuxiang
authors.initials: Y
authors.lastname: Dong
authors.affiliation: Department of Pathology and Microbiology, University of Nebraska Medical Center, 986495 Nebraska Medical Center, Omaha, NE 68198-6495, United States.
authors.forename: Tamara
authors.initials: T
authors.lastname: Lushnikova
authors.affiliation: Department of Pathology and Microbiology, University of Nebraska Medical Center, 986495 Nebraska Medical Center, Omaha, NE 68198-6495, United States.
authors.forename: Radha M
authors.initials: RM
authors.lastname: Golla
authors.affiliation: College of Pharmacy, University of Nebraska Medical Center, 986125 Nebraska Medical Center, Omaha, NE 68198-6125, United States.
authors.forename: Xiaofang
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Pathology and Microbiology, University of Nebraska Medical Center, 986495 Nebraska Medical Center, Omaha, NE 68198-6495, United States. Electronic address: gwang@unmc.edu.
authors.forename: Guangshun
authors.initials: G
authors.lastname: Wang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D015394:Molecular Structure; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D010455:Peptides; D054852:Small Molecule Libraries
keywords: Antimicrobial peptides; Chemical synthesis; Database filtering technology; Peptide mimics