Chair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, Poland.
Institute of Chemical Sciences, Faculty of Chemistry, Maria Curie-Skłodowska University, Maria Curie-Skłodowska Square 2, 20-031 Lublin, Poland.
Molecules. 2024 Aug 11;29(16):3814. doi: 10.3390/molecules29163814.
Nowadays, searching for novel antimicrobial agents is crucial due to the increasing number of resistant bacterial strains. Moreover, cancer therapy is a major challenge for modern medicine. Currently used cytostatics have a large number of side effects and insufficient therapeutic effects. Due to the above-mentioned facts, we undertook research to synthesize novel compounds from the acylhydrazone group aimed at obtaining potential antimicrobial and anticancer agents. As a starting material, we employed hydrazides of 2-, 3- or 4-iodobenzoic acid, which gave three series of acylhydrazones in the condensation reaction with various aldehydes. The chemical structure of all obtained compounds was confirmed by IR, H NMR, and C NMR. The structure of selected compounds was determined by single-crystal X-ray diffraction analysis. Additionally, all samples were characterized using powder X-ray diffraction. The other issue in this research was to examine the possibility of the solvent-free synthesis of compounds using mechanochemical methods. The biological screening results revealed that some of the newly synthesized compounds indicated a beneficial antimicrobial effect even against MRSA-the methicillin-resistant ATCC 43300 strain. In many cases, the antibacterial activity of synthesized acylhydrazones was equal to or better than that of commercially available antibacterial agents that were used as reference substances in this research. Significantly, the tested compounds do not show toxicity to normal cell lines either.
如今，由于耐药菌株数量的增加，寻找新型抗菌剂至关重要。此外，癌症治疗是现代医学的一大挑战。目前使用的细胞抑制剂有许多副作用，疗效不足。鉴于上述事实，我们着手研究合成新型酰腙类化合物，旨在获得有潜力的抗菌和抗癌药物。以 2-、3-或 4-碘苯甲酸的酰肼为起始原料，与各种醛缩合得到了三个系列的酰腙。所有得到的化合物的化学结构都通过 IR、H NMR 和 C NMR 得到了确认。通过单晶 X 射线衍射分析确定了选定化合物的结构。此外，所有样品都进行了粉末 X 射线衍射表征。本研究的另一个问题是研究使用机械化学方法无溶剂合成化合物的可能性。生物筛选结果表明，一些新合成的化合物具有有益的抗菌作用，甚至对耐甲氧西林金黄色葡萄球菌（MRSA-ATCC 43300 株）也有作用。在许多情况下，合成的酰腙的抗菌活性与作为本研究参比物质的市售抗菌剂相当或更好。值得注意的是，测试的化合物对正常细胞系也没有毒性。
