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<p>Malaria remains a major global health challenge, affecting millions worldwide. This study reports the synthesis of two hydrazones (1–2), derived from 5-bromovanillin and different hydrazides, along with their transition metal complexes (3–10), aimed at evaluating their therapeutic potential. The compounds underwent characterization through both spectral and physical analyses, revealing the hexacoordinated stereochemistry of metal chelates. Biological evaluations included antimicrobial, antimalarial, and anti-inflammatory assays using serial dilution, micro-assay, and BSA methods, respectively. The pharmacological assessments highlighted that metal chelates unveiled enhanced therapeutic efficacy in contrary to their ligands. Notably, compounds H<sub>2</sub>L<sup>2</sup> (2) and its complexes (9), (10) emerged as most effective malarial agents with IC<sub>50</sub> value 0.58 ± 0.013, 0.64 ± 0.024&#xa0;µM against <i>P. falciparum.</i> Additionally, the compounds displayed varying degrees of antimicrobial activity, with complexes (5), (9), and (10) exhibiting the strongest efficacy against <i>S. aureus</i> and <i>E. coli</i>, showing MIC values between 0.0075 and 0.0081&#xa0;µmol/mL. Furthermore, the anti-inflammatory evaluation revealed that chelates (9) and (10) exhibited superior activity, with IC<sub>50</sub> values of 7.12 ± 0.053 and 7.62 ± 0.062&#xa0;µM, respectively. Additionally, molecular docking studies against target protein (PDB ID: 1U5A) supported strong binding affinities of H<sub>2</sub>L<sup>2</sup> (2) and its complexes (9–10). Moreover, ADMET study offered compounds’ drug-like properties.</p>

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Hydrazone ligands and their metal chelates: a confluence of spectroscopic, biological, and computational discoveries

  • 期刊论文

  • 发表日期：

    2025年8月28日

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  • Jai Devi,
  • Tanisha Arora,
  • Gita Rani,
  • Meena Rani

摘要

Malaria remains a major global health challenge, affecting millions worldwide. This study reports the synthesis of two hydrazones (1–2), derived from 5-bromovanillin and different hydrazides, along with their transition metal complexes (3–10), aimed at evaluating their therapeutic potential. The compounds underwent characterization through both spectral and physical analyses, revealing the hexacoordinated stereochemistry of metal chelates. Biological evaluations included antimicrobial, antimalarial, and anti-inflammatory assays using serial dilution, micro-assay, and BSA methods, respectively. The pharmacological assessments highlighted that metal chelates unveiled enhanced therapeutic efficacy in contrary to their ligands. Notably, compounds H2L2 (2) and its complexes (9), (10) emerged as most effective malarial agents with IC50 value 0.58 ± 0.013, 0.64 ± 0.024 µM against P. falciparum. Additionally, the compounds displayed varying degrees of antimicrobial activity, with complexes (5), (9), and (10) exhibiting the strongest efficacy against S. aureus and E. coli, showing MIC values between 0.0075 and 0.0081 µmol/mL. Furthermore, the anti-inflammatory evaluation revealed that chelates (9) and (10) exhibited superior activity, with IC50 values of 7.12 ± 0.053 and 7.62 ± 0.062 µM, respectively. Additionally, molecular docking studies against target protein (PDB ID: 1U5A) supported strong binding affinities of H2L2 (2) and its complexes (9–10). Moreover, ADMET study offered compounds’ drug-like properties.