Bench and Byte: Synthesis, DFT, ADMET, and Molecular Docking on a Pair of Antibacterial Schiff Bases Targeting DNA Gyrase

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Authors: Munirah M. Al‐Rooqi, Israa J. Hakeem, Saeed S. Samman, Abdulrahman A. Alsimaree, Mustafa S. Alluhaibi, Abdulaziz M. Almohyawi, Sultan I. Alkubaysi, Ziad Moussa, Jan Mohammad Mir, Saleh A. Ahmed
Cited by: 1
References: 60

Abstract

ABSTRACT Schiff bases are privileged azomethine pharmacophores with diverse bioactivity. In this report, two new hydrazine‐derived Schiff bases, L 1 and L 2, were synthesized. The structures were confirmed by experimental approaches involving IR, UV–vis, 1 H, and 1 3 C NMR spectroscopy and showed strong correlation with theoretical computational predictions. Molecular reactivity was explored using DFT (B3LYP/6‐311G(d,p), SMD/water) through frontier orbitals, electrostatic potential, and global reactivity descriptors. Antibacterial evaluation against Escherichia coli , Staphylococcus aureus , and Pseudomonas aeruginosa showed strain‐selective potency: L 1 was most active against S. aureus and E. coli (MIC 4.9 and 6.5 µg/mL), while L 2 displayed moderate activity against P. aeruginosa (MIC 8.4 µg/mL). Ciprofloxacin remained the strongest reference (MIC 0.049–0.521 µg/mL). Docking with DNA gyrase (PDB ID 6F86) indicated favorable binding for L 1 (−6.4 kcal/mol) and L 2 (−6.0 kcal/mol) vs. ciprofloxacin (−7.0 kcal/mol). ADMET predictions supported acceptable drug‐likeness and low toxicity. These results highlight hydrazine‐based Schiff bases as promising leads for antibacterial design against multidrug resistance.

Fields of Study & Subjects

Metal complexes synthesis and properties Synthesis and biological activity Cancer therapeutics and mechanisms

Publication details

Journal / source
ChemistrySelect
Publisher
Wiley
Volume
11
Issue
6
Publication date
1 February 2026
Language
EN