双核三环己基膦银（I）二硫代氨基甲酸盐，{CyPAg(SCNRR')}的体外抗细菌和时间杀伤评估。
In vitro anti-bacterial and time kill evaluation of binuclear tricyclohexylphosphanesilver(I) dithiocarbamates, {CyPAg(SCNRR')}.
机构信息
Research Centre for Crystalline Materials, School of Science and Technology, Sunway University, No. 5 Jalan Universiti, 47500 Bandar Sunway, Selangor Darul Ehsan, Malaysia; Department of Biological Sciences, School of Science and Technology, Sunway University, No. 5 Jalan Universiti, 47500 Bandar Sunway, Selangor Darul Ehsan, Malaysia.
Research Centre for Crystalline Materials, School of Science and Technology, Sunway University, No. 5 Jalan Universiti, 47500 Bandar Sunway, Selangor Darul Ehsan, Malaysia.
出版信息
J Inorg Biochem. 2019 Mar;192:107-118. doi: 10.1016/j.jinorgbio.2018.12.017. Epub 2019 Jan 6.
Four binuclear phosphanesilver(I) dithiocarbamates, {cyclohexylPAg(SCNRR')} for R = R' = Et (1), CHCH (2), CHCHOH (3) and R = Me, R' = CHCHOH (4) have been synthesised and characterised by spectroscopy and crystallography, and feature tri-connective, μ-bridging dithiocarbamate ligands and distorted tetrahedral geometries based on PS 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 log CFU/mL against S. aureus (MRSA).
四种双核膦银（I）二硫代氨基甲酸盐，{环己基 PAg（SCNRR'）}，其中 R=R'=Et（1），CHCH（2），CHCHOH（3）和 R=Me，R'=CHCHOH（4），已通过光谱学和晶体学进行了合成和表征，并具有三连接的μ桥联二硫代氨基甲酸盐配体和基于 PS 供体的扭曲四面体几何结构。这些化合物的抗细菌活性已针对总共 12 种临床重要病原体进行了评估。根据最小抑菌浓度（MIC）和细胞活力测试（人胚肾细胞，HEK 293），1-4 对革兰氏阳性菌具有特异性活性，同时毒性较低；3 和 4 对耐甲氧西林金黄色葡萄球菌（MRSA）有效。在整个系列中，4 的效果最佳，比标准抗生素氯霉素更有效。时间杀伤实验表明，1-4 对敏感细菌具有时间和浓度依赖性的药代动力学。化合物 4 在 1 和 2×MIC 下对金黄色葡萄球菌（MRSA）表现出快速（2 小时内）杀菌活性，达到最大减少 5.2 log CFU/mL。
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