In Vitro Synthesis, Structure elucidation and its antioxidant properties of Platinum(IV)-hydrazide complexes: Molecular modeling of free-hydrazides suggested as potent lipoxygenase inhibitor.

doi:10.2174/1573406417666210216160941

Paper

In Vitro Synthesis, Structure elucidation and its antioxidant properties of Platinum(IV)-hydrazide complexes: Molecular modeling of free-hydrazides suggested as potent lipoxygenase inhibitor.

Published Feb 16, 2021 · Rooma Badar, U. Ashiq, R. Jamal

Medicinal chemistry (Shariqah (United Arab Emirates))

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Abstract

BACKGROUND Combination of biologically active ligand and metal in one molecule may increase the activity and reduce the toxicity. OBJECTIVES In this study synthesis and characterization of platinum(IV) complexes with bioactive hydrazide ligands is discussed. METHOD Elemental analysis, conductivity measurements and spectroscopic studies were used to elucidate the structure of complexes. RESULTS Our study suggests that hydrazide ligands coordinate with Pt(IV) in bidenate fashion. The platinum(IV) complexes have octahedral geometry with metal to ligand ratio of 1:2. Hydrazide ligands coordinated with central metal platinum(IV) by oxygen of carbonyl group and nitrogen of primary amine. Synthesized complexes exhibited variable DPPH radical scavenging and lipoxygenase inhibition activity. Furthermore, it is also found that Pt(IV)-hydrazide complexes are more potent superoxide and nitric oxide radical scavengers than their uncoordinated hydrazide ligands while in case of lipoxygenase enzyme inhibition, some of the free hydrazide ligands are more active than their respective Pt(IV) complexes. In silico docking technique explores molecular interactions of synthesized ligands in the active site of lipoxygenase enzyme. Predicted docking energies are in good agreement with experimental data suggesting that in silico studies might be useful for discovery of therapeutic candidates. CONCLUSION Structure function relationship demonstrates that the radical scavenging and enzyme inhibition activities of the Pt(IV) compounds are effected by nature of ligand, position of substituent, electronic and steric effects. However, electronic factor seem to play more important role than other factors.

In Vitro Study

Study Snapshot

Platinum(IV)-hydrazide complexes show potential as potent antioxidants and lipoxygenase inhibitors, with electronic factors playing a more important role than other factors.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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In Vitro Synthesis, Structure elucidation and its antioxidant properties of Platinum(IV)-hydrazide complexes: Molecular modeling of free-hydrazides suggested as potent lipoxygenase inhibitor.

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