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

Four compounds, R 3 PAu[S 2 CN(CH 2 CH 2 OH) 2 ], R = Ph ( 1 ) and cyclohexyl ( 2 ), and Et 3 PAuS 2 CNRꞌ 2 , Rꞌ = Rꞌ = Et ( 3 ) and Rꞌ 2 = (CH 2 ) 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. 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. [ABSTRACT FROM AUTHOR]