Bacterial resistance to antimicrobial agents is increasing at an alarming rate globally and requires new lead compounds for antibiotics. In this study, N-phenyl-N-nitroso hydroxylamine (cupferron) and its derivatives have been synthesised using readily available starting materials. The compounds were obtained in high yield and purity. They show activity towards a range of Gram-positive and Gram-negative pathogenic bacteria, with minimum inhibitory concentration (MIC) values as low as 2 μg.mL⁻¹ against the tested organisms, especially for Gram-positive species. Toxicity studies on the lead compound 3b indicate insignificant effects on healthy cell lines. Molecular docking studies on the lead compound identify possible binding modes of the compound, and the results obtained correlate with those of in vitro and MIC studies. The lead compound shows excellent drug-likeness properties.

全球细菌对抗菌剂的耐药性正在以惊人的速度增加，需要新的抗生素先导化合物。在这项研究中，N-苯基-N-亚硝基羟胺（铜氨）及其衍生物是使用容易获得的起始材料合成的。化合物以高产率和纯度获得。它们显示出对一系列革兰氏阳性和革兰氏阴性病原菌的活性，对测试生物体的最小抑制浓度 (MIC) 值低至 2 μg.mL ^-1，特别是对革兰氏阳性菌种。先导化合物3b的毒性研究表明对健康细胞系的影响微不足道。先导化合物的分子对接研究确定了该化合物可能的结合模式，获得的结果与体外和 MIC 研究的结果相关。该先导化合物显示出优异的药物相似性。