title: In vitro antibacterial and time kill evaluation of mononuclear phosphanegold(I) dithiocarbamates.
abstract: Four compounds, R3PAu[S2CN(CH2CH2OH)2], R=Ph (1) and cyclohexyl (2), and Et3PAuS2CNRꞌ2, Rꞌ=Rꞌ=Et (3) and Rꞌ2=(CH2)4(4), have been evaluated for antibacterial activity against a panel of 24 Gram positive (8) and Gram negative (16) bacteria. Based on minimum inhibitory concentration (MIC) scores, compounds 1 and 2 were shown to be specifically potent against Gram positive bacteria whereas compounds 3 and, to a lesser extent, 4 exhibited broad range activity. All four compounds were active against methicillin resistant Staphylococcus aureus (MRSA). Time kill assays revealed the compounds to exhibit both time- and concentration-dependent pharmacokinetics against susceptible bacteria. Each compound was bactericidal against one or more bacteria with 3 being especially potent after 8h exposure; compounds 1 and 3 were bactericidal against MRSA. Compound 3 was the most effective bactericide across the series especially toward B. subtilis, S. saprophyticus, A. hydrophila, P. vulgaris, and V. parahaemolyticus. This study demonstrates the potential of this class of compounds as antibacterial agents, either broad range or against specific bacteria.
authors.affiliation: Department of Biomedical Science, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia.
authors.forename: Bao-Jing
authors.initials: BJ
authors.lastname: Chen
authors.affiliation: Department of Chemistry, University of Malaya, 50603 Kuala Lumpur, Malaysia.
authors.forename: Nazzatush Shimar
authors.initials: NS
authors.lastname: Jamaludin
authors.affiliation: Department of Biomedical Science, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia.
authors.forename: Chai-Hoon
authors.initials: CH
authors.lastname: Khoo
authors.affiliation: Department of Biomedical Science, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia.
authors.forename: Tian-Hong
authors.initials: TH
authors.lastname: See
authors.affiliation: Department of Biomedical Science, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia.
authors.forename: Jiun-Horng
authors.initials: JH
authors.lastname: Sim
authors.affiliation: Department of Biomedical Science, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia. Electronic address: ykcheah@medic.upm.edu.my.
authors.forename: Yoke-Kqueen
authors.initials: YK
authors.lastname: Cheah
authors.affiliation: Department of Chemistry, University of Malaya, 50603 Kuala Lumpur, Malaysia.
authors.forename: Siti Nadiah Abdul
authors.initials: SN
authors.lastname: Halim
authors.affiliation: Department of Biological Sciences, Faculty of Science and Technology, Sunway University, 47500 Bandar Sunway, Selangor Darul Ehsan, Malaysia.
authors.forename: Hoi-Ling
authors.initials: HL
authors.lastname: Seng
authors.affiliation: Research Centre for Crystalline Materials, Faculty of Science and Technology, Sunway University, 47500 Bandar Sunway, Selangor Darul Ehsan, Malaysia. Electronic address: edwardt@sunway.edu.my.
authors.forename: Edward R T
authors.initials: ER
authors.lastname: Tiekink
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000254:growth & development*; D050607:Organogold Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013859:Thiocarbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D050607:Organogold Compounds; D013859:Thiocarbamates
keywords: Antimicrobial; Dithiocarbamate; Phosphanegold(I) compounds; Thiolate; Time kill assay