Synthesis, anticonvulsant, antioxidant and binding interaction of novel N-substituted methylquinazoline-2,4(1H, 3H)-dione derivatives to bovine serum albumin: A structure-activity relationship study

Prashanth, M. K. and Madaiah, M. and Revanasiddappa, H. D. and Veeresh, B. (2013) Synthesis, anticonvulsant, antioxidant and binding interaction of novel N-substituted methylquinazoline-2,4(1H, 3H)-dione derivatives to bovine serum albumin: A structure-activity relationship study. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy, 110. pp. 324-332.

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Official URL: http://doi.org/10.1016/j.saa.2013.03.064

Abstract

A novel class of N-substituted glycosmicine derivatives was synthesized, and their anticonvulsant, antioxidant activity and interaction with bovine serum albumin (BSA) were evaluated. The synthesized compounds 4a-j were examined for anticonvulsant activity by maximal electroshock induced seizures (MESs) test and their neurotoxic effects were determined by rotorod test in mice. The structure-activity relationships (SARs) of these compounds were also investigated. Compounds 4d, 4g, 4i and 4j were found to have good protective effect from seizure. The in vitro antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical scavenging assay. The interaction between novel N-substituted methylquinazoline-2,4(1H, 3H)-dione (NMQ) and BSA was analyzed by fluorescence and ultraviolet spectroscopy at 304 K under simulative physiological conditions. BSA fluorescence quenched by NMQ is discussed according to the Stern-Volmer equation. The binding constant and binding sites of NMQ with BSA were calculated. According to Forster non-radiation energy transfer theory, the binding distance (r) between NMQ and BSA was calculated.

Item Type: Article
Uncontrolled Keywords: 1, 1 diphenyl 2 picrylhydrazyl, 2, 2-diphenyl-1-picrylhydrazyl, animal, Animals, Anti-oxidant activities, Anticonvulsant activity, Anticonvulsants, anticonvulsive agent, antioxidant, Antioxidants, article, Binding energy, Binding interaction, binding site, Binding Sites, Biphenyl Compounds, biphenyl derivative, Body fluids, Bovine, bovine serum albumin, Bovine serum albumins, cattle, Cattle, chemistry, Energy transfer, Fluorescence, Fluorescence spectroscopy, Mammals, metabolism, Mice, mouse, Oxygen, Physiological condition, Picrates, picric acid, protein binding, Protein Binding, quinazoline derivative, Quinazolines, seizure, Seizures, Serum Albumin, spectrofluorometry, Spectrometry, Stern-Volmer equation, structure activity relation, Structure activity relationships, Structure-Activity Relationship, Substitution reactions, superoxide, Superoxides, Ultraviolet spectroscopy
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar
Date Deposited: 19 Oct 2019 07:23
Last Modified: 19 Oct 2019 07:23
URI: http://eprints.uni-mysore.ac.in/id/eprint/9162

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