Hydrazone analogues with promising antibacterial profiles: Synthesis, morphology, in vitro and in silico approaches

The emergence of resistance to antibacterial drugs remains an important global threat that necessitates an urgent need for the discovery of alternative drugs. This study was undertaken to synthesize some novel nitroaryl/heteroaryl hydrazone derivatives as potential antibacterial agents. After synthesizing by a simple reaction between quinoline/quinazoline hydrazine and nitroaryl/heteroaryl aldehydes, all the compounds were screened for their antibacterial activities, cytotoxicity and in silico investigations. The compound, 2‐(4‐nitrobenzylidene)‐1‐(quinazolin‐4‐yl)hydrazine (1b), displayed significant antimicrobial activity against several susceptible and resistant bacteria without any cytotoxicity. Moreover, scanning electron microscopy (SEM) revealed the complete destruction of Staphylococcus aureus and Escherichia coli following exposure to this compound after 2 h exposure. The in silico studies confirmed the better binding energy of these compounds in comparison with the reference drugs in complex with topoisomerase IV and bacterial ribosomal receptor. Compound 1b can be considered a promising lead compound for the development of broad‐spectrum antibacterial medications after further studies. Significance and Impact of the Study: Bacterial resistance development against commercial antibiotics has become one of the most significant global problems. There is a strong demand for the discovery of novel classes of antibiotics with high efficiency, low dose, no toxicity and affordable cost. According to the results described in this research, non‐toxic nitrobenzylidene(quinazolin‐4‐yl)hydrazines (compounds 1b and 2b) can be considered promising medications for the treatment of infectious diseases owing to their proper activity against various susceptible and resistant bacteria. Furthermore, they can become industrialized because of their convenient and high‐yield synthesis.