Synthesis, Antibacterial, Docking and Anticancer Evaluation of N-Substituted Benzoyl Derivatives

Abstract

A series of N-benzoylated ligands incorporating three different benzoyl groups 2,2'-(benzoyliminodiethylene)-4substituted phenols (L 1,4,7 ), 2,2'-(4-nitrobenzoyliminodiethylene)-4-substituted phenols (L 2,5,8 ) and 2,2'-(3,5dinitrobenzoyliminodiethylene)-4-substituted phenols (L 3,6,9 ) were synthesized and characterized by IR, 1 H NMR, 13 C NMR and mass spectroscopy. The In vitro antibacterial activity of investigated ligands were tested against human pathogenic bacteria such as four Gram (-) Enterococcus faecalis, Pseudomonas aeruginosa, Staphylococcus aureus, Vibrio cholera, Vibrio harveyi and two Gram (+) Staphylococcus aureus, Streptococcus mutans. Furthermore, docking studies were undertaken to gain insight into the possible binding mode of these compounds with the binding site of the topoisomerase II (PDB: 4FM9) enzyme which is involved in DNA superhelicity and chromosome seggregation. The Nbenzoylated derivatives L 5, 7, 8 have significant anticancer activity as Topoisomerase inhibitors. The ligands L 5 and L 8 were tested for their anticancer activity against human liver adenocarcinoma (HepG2) cell line with the MTT assay.

Multi-target activity of copper complexes: Antibacterial, DNA binding, and molecular docking with SARS-CoV-2 receptor

“…The peak at 443.52 confirms the molecular weight of the ligand and the peak at 465.43 denotes the molecular weight of the ligand plus sodium and the peak at 886.45 is the dimer form of the ligand. Both NMR and ESI-MS spectral data along with elemental analysis have confirmed the formation of ligands and their purity [ 19 ].

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“…The ligands H 2 L 1–3 and similar type of other ligands was synthesized and reported by our group [ 16 , 17 , 19 ].…”