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Novel ferrocenyl chalcone derivatives as antibacterial agents: is there a solution to the problem?
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-05-17 , DOI: 10.1007/s00044-021-02738-1
Elecia J. Henry , Charles Thomas Bennett , Michael Collins , John P. Cassella

Increased infection spread is partly facilitated by reduced new drug development. Because of their antimicrobial properties, ferrocenyl chalcone derivatives were assessed in a previous study. However, dilutions of stock ferrocenyl chalcone solution with Mueller–Hinton broth (MHB) resulted in particle formation, and a colour change from deep red to dark-brown. Results of the current study confirmed particle formation, which suggested the chelation of casein hydrolysate, a component of MHB, by iron ion. After solubilisation in dimethyl sulfoxide (DMSO), each of the iodine-containing compounds, also changed from deep red to dark-brown. Mean rates of colour change (RA) in polypropylene tubes at 37 °C were the highest (0.0102 ± 0.0005 ΔA/min−0.0041 ± 0.0009 ΔA/min) while the same observed reaction in borosilicate glass tubes 21 °C ± 1 were the lowest (0.0024 ± 0.0007 ΔA/min−0.0021 ± 0.0003 ΔA/min). Antimicrobial activity of two randomly selected ferrocenyl chalcone compounds (hexyl and heptyl) was unaffected after colour change occurred (0.016−0.125 mg/ml). Although these findings potentially indicate that short-term storage of antimicrobials is unaffected, further work is required to assess whether antimicrobial activity is affected by longer storage conditions.



中文翻译:

新型二茂铁基查尔酮衍生物作为抗菌剂:有解决方案吗?

减少新药开发可部分促进感染传播的增加。由于它们的抗菌特性,在先前的研究中评估了二茂铁基查耳酮衍生物。但是,用Mueller-Hinton肉汤(MHB)稀释二茂铁基查尔酮储备溶液会导致颗粒形成,并且颜色从深红色变为深棕色。当前研究的结果证实了颗粒的形成,这表明酪蛋白水解产物(MHB的一种成分)与铁离子螯合。在二甲基亚砜(DMSO)中溶解后,每种含碘化合物也从深红色变为深棕色。聚丙烯管在37°C时的平均颜色变化率(RA)最高(0.0102±0.0005ΔA/ min-0.0041±0。0009ΔA/ min)而在21°C±1的硼硅玻璃管中观察到的反应最低(0.0024±0.0007ΔA/ min-0.0021±0.0003ΔA/ min)。发生颜色变化(0.016-0.125 mg / ml)后,两种随机选择的二茂铁基查耳酮化合物(己基和庚基)的抗菌活性未受影响。尽管这些发现可能表明抗菌药物的短期储存不受影响,但仍需要进一步的工作来评估抗菌活性是否受到较长储存条件的影响。

更新日期:2021-05-17
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