Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Dokki, Cairo 12622, Egypt.
Radioisotopes Department, Nuclear Research Centre, Egyptian Atomic Energy Authority, Cairo 13759, Egypt.
Molecules. 2022 Jun 4;27(11):3613. doi: 10.3390/molecules27113613.
Novel 1,3,4-thiadiazole derivatives were synthesized through the reaction of methyl 2-(4-hydroxy-3-methoxybenzylidene) hydrazine-1-carbodithioate and the appropriate hydrazonoyl halides in the presence of a few drops of diisopropylethylamine. The chemical structure of the newly fabricated compounds was inferred from their microanalytical and spectral data. With the increase in microbial diseases, fungi remain a devastating threat to human health because of the resistance of microorganisms to antifungal drugs. COVID-19-associated pulmonary aspergillosis (CAPA) and COVID-19-associated mucormycosis (CAM) have higher mortality rates in many populations. The present study aimed to find new antifungal agents using the disc diffusion method, and minimal inhibitory concentration (MIC) values were estimated by the microdilution assay. An in vitro experiment of six synthesized chemical compounds exhibited antifungal activity against Rhizopus oryzae; compounds with an imidazole moiety, such as the compound 7, were documented to have energetic antibacterial, antifungal properties. As a result of these findings, this research suggests that the synthesized compounds could be an excellent choice for controlling black fungus diseases. Furthermore, a molecular docking study was achieved on the synthesized compounds, of which compounds 2, 6, and 7 showed the best interactions with the selected protein targets.
新型 1,3,4-噻二唑衍生物是通过在少量二异丙基乙胺存在下,使甲基 2-(4-羟基-3-甲氧基苯亚甲基)腙-1-碳二硫代酸酯与适当的酰肼卤反应合成的。新合成化合物的化学结构是根据其微量分析和光谱数据推断出来的。随着微生物疾病的增加,由于微生物对抗真菌药物的耐药性,真菌仍然对人类健康构成严重威胁。COVID-19 相关肺曲霉病(CAPA)和 COVID-19 相关毛霉病(CAM)在许多人群中的死亡率更高。本研究旨在使用圆盘扩散法寻找新的抗真菌剂,并通过微量稀释法估计最小抑菌浓度(MIC)值。对六种合成化学化合物的体外实验显示对根霉有抗真菌活性;具有咪唑部分的化合物,如化合物 7,被证明具有有效的抗菌、抗真菌特性。基于这些发现,本研究表明合成化合物可能是控制黑霉菌病的绝佳选择。此外,还对合成化合物进行了分子对接研究,其中化合物 2、6 和 7 与所选蛋白靶标表现出最佳相互作用。