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  • In vitro anti-bacterial and...
    Tan, Yi Jiun; Tan, Yee Seng; Yeo, Chien Ing; Chew, Jactty; Tiekink, Edward R.T.

    Journal of inorganic biochemistry, 03/2019, Letnik: 192
    Journal Article

    Four binuclear phosphanesilver(I) dithiocarbamates, {cyclohexyl3PAg(S2CNRR′)}2 for R = R′ = Et (1), CH2CH2 (2), CH2CH2OH (3) and R = Me, R′ = CH2CH2OH (4) have been synthesised and characterised by spectroscopy and crystallography, and feature tri-connective, μ2-bridging dithiocarbamate ligands and distorted tetrahedral geometries based on PS3 donor sets. The compounds were evaluated for anti-bacterial activity against a total of 12 clinically important pathogens. Based on minimum inhibitory concentration (MIC) and cell viability tests (human embryonic kidney cells, HEK 293), 1–4 are specifically active against Gram-positive bacteria while demonstrating low toxicity; 3 and 4 are active against methicillin resistant S. aureus (MRSA). Across the series, 4 was most effective and was more active than the standard anti-biotic chloramphenicol. Time kill assays reveal 1–4 to exhibit both time- and concentration-dependent pharmacokinetics against susceptible bacteria. Compound 4 demonstrates rapid (within 2 h) bactericidal activity at 1 and 2 × MIC to reach a maximum decrease of 5.2 log10 CFU/mL against S. aureus (MRSA). Binuclear phosphanesilver(I) dithiocarbamates species display anti-bacterial against several Gram positive bacteria with {cyclohexyl3PAgS2CN(Me)CH2CH2OH}2 being bactericidal against S. aureus (MRSA). Display omitted •Cyclohexylphosphanesilver(I) dithiocarbamates exhibit anti-bacterial activity.•All compounds are active against Gram positive bacteria.•Species with hydroxyethyl substituents are more potent than alkyl analogues.•A variety of bacteriostatic and bactericidal activities are observed.•{(Cyclohexyl)3PAgS2CN(Me)CH2CH2OH}2 is the most promising candidate for further research.