Synthesis, characterization and biological activities of cetirizine analogues. Issue 4 (2011)

• Record Type: Journal Article
• Authors: Sultana Sultana, Najma Najma; Arayne Arayne, M. Saeed M. Saeed; Shamshad Shamshad, Hina Hina; Mirza Mirza, Agha Zeeshan Agha Zeeshan; Naz Naz, Malik Asia Malik Asia; Fatima Fatima, Beenish Beenish; Asif Asif, M. M.; Mesaik Mesaik, M. Ahmed M. Ahmed
• Is Part Of: Spectroscopy. Volume 26:Issue 4/5(2011)
• Page Start: 317
• Page End: 328
• Publication Date: 2011
• Subjects: Cetirizine -- oxidative burst -- anti-inflammatory activities -- H_1-receptor antagonist
• DOI: 10.3233/SPE-2011-0537
• Languages: English
• ISSNs: 0712-4813

Abstract

Abstract : 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, 1 H 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.