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Relationship Structure – Activity. Phenolic Group and Aromatic Electron- Withdrawing Effect of Substituents as Pharmacophores for the Antipyretic Activity

HomeRelationship Structure – Activity. Phenolic Group and Aromatic Electron- Withdrawing Effect of Substituents as Pharmacophores for the Antipyretic Activity

Research Article

Relationship Structure - Activity. Phenolic Group and Aromatic Electron- Withdrawing Effect of Substituents as Pharmacophores for the Antipyretic Activity

J.N.Molisho , M.Masamba

Corresponding Author : Joseph Ngongo Molisho,

Département de chimie, Faculté des Sciences,Université de Kinshasa,B.P.190 Kinshasa XI, DR CONGO

Email ID : molishon@yahoo.fr

Received : 2015-09-23 Accepted : 2015-10-30 Published : 2015-10-30

Abstract : 2-Hydroxy-5-nitro benzoic acid 1 has been synthesized from acetyl salicylic acid known as aspirin. The synthesized compound has been characterized using proton, carbon-13 Nuclear Magnetic Resonance data. The evaluation of its in vivo antipyretic activities above the Wistars rats shows that the derivative 1 is most active than its analogue aspirin. The derivative 1 shows an average temperature decrease of 1,4°C at the minimal concentration of 0,125 mol/l against Plasmodium bergei inoculated to the Wistars rats, whereas aspirin doesn’t show any activity under the same conditions. The higher antipyretic activity of the derivative 1 is explained by the pharmacophore character of the phenolic group reinforced with intramolecular H-bonds and the aromatic electron-withdrawing effect of substituents

Keywords : Aspirin derivative, higher in vivo antipyretic activity, phenolic group, electron-withdrawing substituents, pharmacophores for antipyretic activity.

Citation : J.N.Molisho et al.. (2015) T Relationship Structure - Activity. Phenolic Group and Aromatic Electron- Withdrawing Effect of Substituents as Pharmacophores for the Antipyretic Activity. j. of Physical and Chemical Sciences.V3I3.010. DOI : 10.5281/zenodo.999911

Copyright : © 2015 J.N.Molisho.. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Journal of Physical and Chemical Sciences

ISSN : 2348-327X

Volume 3 / Issue 3

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