In vitro antibacterial and time kill evaluation of mononuclear phosphanegold(I) dithiocarbamates

Abstract

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.

Properties of Poly-γ-Glutamic Acid Producing-Bacillus Species Isolated From Ogi Liquor and Lemon-Ogi Liquor

“…The initial decrease varied with the pathogen and type of γPGA used. Previous authors have similar reports on the increase in growth of pathogens at certain intervals after MIC exposure (Sim et al, 2014; Chen et al, 2016; Appiah et al, 2017). The log-reduction and subsequent regrowth suggest that the antimicrobial effect of γPGA is concentration and time-dependent.…”

“…Time-kill assay of γPGA was carried out according to the recommended CLSI standard as described by Chen et al (2016). Bacteriostatic effect of PGA was interpreted as < 3log 10 , while bactericidal effect as ≥ 3 log 10 in viable colony relative to initial inoculum.…”

Crystal structure of bis[μ2-(N,N-diethylcarbamodithioato-κS:κS,κS′)]-bis(triethylphosphine-P)-di-silver(I), C22H50Ag2N2P2S4

“…In response to the exciting anti-bacterial activity, usually against Gram-positive bacteria, exhibited by phosphanegold(I) dithiocarbamate compounds, R 3 PAu(S 2 CNR′R′′) [5], attention turned to related copper(I) and silver(I) species [6,7] of which compounds of the general Cy 3 PAg(S 2 CNR′R′′) proved most promising [7]. Complementing biological studies, are structural investigations which reveal the monomer formulation to be an over-simplification.…”

1-(2-Hydroxyethyl)imidazolidine-2-thione

“…Such cyclization reactions have been documented in dithiocarbamate chemistry as being a convenient method to form 1-alkyl-2-imidazolidinethiones [8,9], suggesting the organotin reagent is not required for the synthesis. The motivation for the original reaction was to generate bioactive organotin dithiocarbamate compounds inspired by their biological activity, primarily anti-cancer and anti-microbial [10], and as a result of the recent reports of the potential anti-cancer (gold [11], bismuth [12], and zinc [13]) and anti-microbial (copper, silver [14] and gold [15,16]) activities of metal hydroxyethyl-substituted dithiocarbamate compounds, the biological activity of metal dithiocarbamates has been reviewed [17]. Herein, the spectroscopic characterization and X-ray crystal structure determination of 1 are reported.…”

“…The molecular structure of 1 showing atom labeling and displacement ellipsoids at the 70% probability level. Selected geometric parameters: C1=S1 = 1.6996(13), C1-O5 = 1.4261(16), C1-N1 = 1.3385(17), C2-N1 = 1.4590(18), C1-N2 = 1.3356(16), C3-N2 = 1.4665(16), C4-N2 = 1.4551(16), and C2-…”