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

Author:

Nabizadeh M.12,Naimi-Jamal M.R.1,Rohani M.34,Azerang P.2,Tahghighi A.2ORCID

Affiliation:

1. Research Laboratory of Green Organic Synthesis and Polymers Department of Chemistry Iran University of Science and Technology Tehran Iran

2. Medicinal Chemistry Laboratory Department of Clinical Research Pasteur Institute of Iran Tehran Iran

3. Department of Microbiology Pasteur Institute of Iran Tehran Iran

4. Research Center for Emerging and Reemerging Infectious Diseases Pasteur Institute of Iran Tehran Iran

Abstract

Abstract 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.

Publisher

Oxford University Press (OUP)

Subject

Applied Microbiology and Biotechnology

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