The in vitro antibacterial activity of a series of phosphanegold(I) dithiocarbamates, R 3 PAu[S 2 CN (iPr)CH 2 CH 2 OH] where R = Ph (2), Cy (3) and Et (4), against 25 strains of Gram-positive and Gram-negative bacteria were determined through the disk diffusion method, the determination of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) and by time-kill assay. Compounds 2 and 3 have been shown to be specifically active against the tested Gram-positive bacteria, with MIC values ranging from 7.81 to 125 μg/ml. Compound 4 has a broadspectrum activity against 24 strains of Gram-positive and Gram-negative bacteria, with MIC values ranging from 0.98 to 1,000 μg/ml. Noteworthy was that 4, with a very low MIC value of 0.98 μg/ml, is particularly effective against methicillin-resistant Staphylococcus aureus (MRSA) and Bacillus sp., as effective as the standard antibiotic ciprofloxacin. In time-kill studies, the bacteriostatic and bactericidal activities of the tested compounds towards susceptible strains were similar to their characteristics determined by MBC/MIC ratios. In the time-kill assay, 2 and 3 showed only bactericidal activity towards the susceptible strains tested, whereas 4 revealed varying degrees of bactericidal and bacteriostatic activities, results indicating different antibacterial mechanisms are involved.
Soy sauce is a traditional liquid condiment that originated in China over 2,500 years ago and remains a key seasoning ingredient in Asian countries (Zhu & Tramper, 2013). It has different designations depending on the country, shoyu in Japan, chiang-yu (or -yi) in China, kicap in Indonesia and Malaysia, kunjang in Korea, toyo in the Philippines, and see-ieu in Thailand (Otoole, 1997). In addition
Four compounds, R3PAu[S2CN(CH2CH2OH)2], R = Ph (1) and Cy (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 8 h 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. hydrophilia, 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.
Keywords: Copper(I) / silver(I) / dithiocarbamate / crystal structure analysis / X-ray diffraction
Abstract.The crystal and molecular structures of (Ph3P)2M[S2CN(Me)CH2CH2OH], M = Cu, isolated as a 1:1 dichloromethane solvate (1.CH2Cl2), and M = Ag (4) show the central metal atom to be coordinated by a symmetrically (1.CH2Cl2) and asymmetrically chelating (4) dithiocarbamate ligand. The distorted tetrahedral geometries are completed by two PPh3 ligands. The presence of hydroxyl-O-H … S(dithiocarbamate) hydrogen bonds leads to centrosymmetric dimeric aggregates in each crystal structure. In the molecular packing of 1.CH2Cl2, channels comprising 1 are formed via aryl-C-H … O interactions with the solvent molecules associated with the walls of the channels via methylene-C-H … S, π(aryl) interactions. For 4, the dimeric aggregates are connected via a network of aryl-C-H … π(aryl) interactions. Preliminary screening for antimicrobial activity was conducted. The compounds were only potent against Gram-positive bacteria. Some further selectivity in activity was noted. Most notably, all compounds were active against methicillin resistant Staphylococcus aureus.
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