Relationship 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. 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.

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