title: Evaluation of 4,5-disubstituted-2-aminoimidazole-triazole conjugates for antibiofilm/antibiotic resensitization activity against MRSA and Acinetobacter baumannii.
abstract: A library of 4,5-disubstituted-2-aminoimidazole-triazole conjugates (2-AITs) was synthesized, and the antibiofilm activity was investigated. This class of small molecules was found to inhibit biofilm formation by methicillin-resistant Staphylococcus aureus (MRSA) at low-micromolar concentrations; 4,5-disubstituted-2-AITs were also able to inhibit and disperse Acinetobacter baumannii biofilms. The activities of the lead compounds were compared against the naturally occurring biofilm dispersant cis-2-decenoic acid and were revealed to be more potent. The ability of selected compounds to resensitize MRSA to traditional antibiotics (resensitization activity) was also determined. Lead compounds were observed to resensitize MRSA to oxacillin by 2-4-fold.
authors.affiliation: Department of Chemistry, North Carolina State University, Raleigh, NC 27695-8204, USA.
authors.forename: Zhaoming
authors.initials: Z
authors.lastname: Su
authors.forename: Lingling
authors.initials: L
authors.lastname: Peng
authors.forename: Roberta J
authors.initials: RJ
authors.lastname: Worthington
authors.forename: Christian
authors.initials: C
authors.lastname: Melander
mesh_terms: D040981:Acinetobacter baumannii / Q000187:drug effects* / Q000502:physiology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018441:Biofilms / Q000187:drug effects*; D007093:Imidazoles / Q000737:chemistry*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects* / Q000502:physiology; D010068:Oxacillin / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D007093:Imidazoles; D014230:Triazoles; C014973:2-aminoimidazole; D010068:Oxacillin