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%20%20%20%20Relationship%20Structure%20-%20Activity.%20Phenolic%20Group%20and%20Aromatic%20Electron-%20Withdrawing%20Effect%20of%20Substituents%20as%20Pharmacophores%20for%20the%20Antipyretic%20Activity
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

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


Corresponding author :

Joseph Ngongo Molisho,
Tel: 00243-812338094,
Email:

Received: September 23, 2015,   Accepted: October 30, 2015,   Published:


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: 10.15297/JPCS.V3I3.03


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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      Journal of Physical and Chemical Sciences