title: A study of the antimicrobial activity of selected synthetic and naturally occurring quinolines.
abstract: The antimicrobial activities of 60 naturally occurring and synthetic quinolines were studied. The quinolines were organised into seven structural subgroups and, using an in-house microtitre assay, were tested against a range of gram-positive and gram-negative bacteria, including a hospital isolate of meticillin-resistant Staphylococcus aureus (MRSA). The quinolines exhibiting good bioactivity [i.e. low minimum inhibitory concentration (MIC)] against two S. aureus strains were then assessed for their antimicrobial activity against a range of eight clinically isolated MRSA strains. The study showed that 30 of the tested compounds displayed antimicrobial activity, mostly against gram-positive bacteria. The effects of substituent groups on the bioactivity of these quinolines have also been discussed. The quinoline 4-hydroxy-3-iodo-quinol-2-one (11) exhibited significant antimicrobial activity, being active against the MRSA clinical isolates with MIC values comparable with the antibiotic vancomycin used in the treatment of MRSA infections. In particular, 4-hydroxy-3-iodo-quinol-2-one (11) showed MIC values of 0.097 microg/mL against an Irish hospital MRSA-1 strain and 0.049 microg/mL against a distinct MRSA strain as well as a non-typeable MRSA strain.
authors.affiliation: School of Biomedical Sciences, University of Ulster, Cromore Road, Coleraine, Co. Derry, Northern Ireland BT52 1SA, UK.
authors.forename: F
authors.initials: F
authors.lastname: O'Donnell
authors.forename: T J P
authors.initials: TJ
authors.lastname: Smyth
authors.forename: V N
authors.initials: VN
authors.lastname: Ramachandran
authors.forename: W F
authors.initials: WF
authors.lastname: Smyth
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D011804:Quinolines