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Volume 26, Issue 4-5, Pages 317-328

Synthesis, characterization and biological activities of cetirizine analogues

Najma Sultana,1 M. Saeed Arayne,2 Hina Shamshad,1 Agha Zeeshan Mirza,2,4 Malik Asia Naz,1 Beenish Fatima,3 M. Asif,3 and M. Ahmed Mesaik3

1Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan
2Department of Chemistry, University of Karachi, Karachi, Pakistan
3Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan
4Department of Chemistry, University of Karachi, Karachi-75270, Karachi, Pakistan

Copyright © 2011 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Cetirizine second generation H1-receptor antagonist is an acid metabolite of hydroxyzine. Present work was based on six new analogues of cetirizine having nucleophilic substitution reaction synthetic pathway. The reactions were proceeded by replacing the scaffold on the cetirizine moiety using nucleophilic substitution reaction. The structures of analogues were confirmed using UV, IR, 1H NMR and mass spectroscopic techniques. The analogues were tested for the anti-inflammatory activities on cellular immune response. Oxidative burst response of phagocytes after exposure to the analogues was found to exhibit moderate to significant inhibitory activity (23 to <3.1). However, the compounds as MPC and PPC also showed remarkable inhibitory effect on PHA activated T-cells response and may prove to be lead compounds in therapeutic world.