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1.
Biometals ; 30(6): 873-891, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-28994011

RESUMEN

The present study explores the synthesis and inhibitory potential of vanadium(V) complexes of hydrazides (1c-12c) against oxidative enzymes including xanthine oxidase and lipoxygenase (LOX). In addition, non-enzymatic radical scavenging activities of these complexes were also determined. On the basis of spectral, elemental and physical data, synthesized vanadium(V) complexes are tentatively assigned to have an octahedral geometry with two hydrazide ligands and two oxo groups forming a negatively charged sphere complex with ammonium as counter ion. This is further verified by the conductivity studies of the complexes. Results show that hydrazide ligands (1-12) and their respective vanadium(V) complexes (1c-12c) posses scavenging and inhibition potential against DPPH and LOX, respectively. However, contrary to that uncoordinated ligands showed no activity against nitric oxide, superoxide and xanthine oxidase whereas their complexes showed varying degree of activity. These studies indicate that geometry of complex, nature and position of substituent groups play a vital role in scavenging and inhibition potential of these compounds.


Asunto(s)
Antioxidantes/farmacología , Inhibidores Enzimáticos/farmacología , Compuestos de Vanadio/química , Compuestos de Vanadio/farmacología , Antioxidantes/química , Compuestos de Bifenilo/química , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Evaluación Preclínica de Medicamentos/métodos , Inhibidores Enzimáticos/química , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Hidrazinas/química , Ligandos , Inhibidores de la Lipooxigenasa/química , Inhibidores de la Lipooxigenasa/farmacología , Espectroscopía de Resonancia Magnética , Óxido Nítrico/química , Óxido Nítrico/metabolismo , Picratos/química , Espectrofotometría Infrarroja , Superóxido Dismutasa/antagonistas & inhibidores , Superóxido Dismutasa/metabolismo , Vanadio/química , Xantina Oxidasa/antagonistas & inhibidores
2.
Med Chem ; 11(8): 798-806, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25827721

RESUMEN

Acid hydrazides are vital chemical entities due to their biological activities. Upon complexation with certain metal ions, their biological activities are known to be positively enhanced. The present work describes the synthesis of Cr(III)-hydrazide complexes, and their structural, spectroscopic and antioxidant properties to reveal their chemistry and biochemistry. Physical (magnetic moment, conductivity measurements), analytical (C, H, N and Cr analysis) and spectral (EI-Mass, FTIR) techniques are used for the characterization of synthesized compounds. All Cr(III)-hydrazide complexes exhibit octahedral geometry with general formula [Cr(L)2(H2O)2]Cl3. In these complexes, the hydrazide ligands are coordinated via carbonyl oxygen and terminal amino nitrogen in a bidentate fashion. All Cr(III)-hydrazide complexes were screened for in vitro diphenyldipicryl hydrazine (DPPH), superoxide dismutase and nitric oxide radical scavenging activities. Majority of the Cr(III)-hydrazide complexes were found to be more potent scavengers than their uncoordinated hydrazide ligands. This study demonstrates an interesting structure-activity relationship (SAR) which is presented here.


Asunto(s)
Antioxidantes/química , Cromo/química , Hidrazinas/química , Compuestos Organometálicos/química , Antioxidantes/síntesis química , Ligandos , Compuestos Organometálicos/síntesis química , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta
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