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,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.
Highlights
In recent years research work has been carried out for the synthesis of potent compounds which could be used to treat allergic and inflammatory disorders simultaneously [13,15]
The reaction mechanism for the formation of cetirizine derivatives was considered to be proceeded via attack by the lone pairs present on nitrogen of thiourea, thioacetamide, pheylenediamine, naphthylamine and pthalamide, nitrogen acts as a nucleophile and attacks the carboxyl carbon of the acid which leads to the formation of an alkoxide ion
New functional groups were attached to the cetirizine molecule and their antiinflammatory effects were evaluated
Summary
In recent years research work has been carried out for the synthesis of potent compounds which could be used to treat allergic and inflammatory disorders simultaneously [13,15] Larsson and his coworkers [8] linked the histamine H1-receptor antagonist cetirizine to NO-releasing spacer groups. The compounds selected for these studies were chosen on the basis of their anti-inflammatory activities such as thiourea [1], acetamide [7], phenylenediamine [17], naphthylamine [3] This method allowed the introduction of a variety of substituents such as α-napthylamine, m-phenelendiamine, p-phenelendiamine, thiourea, thioacetaamide and phthalimide into the core structure of cetirizine, at carboxylic group, in a quick and simple way. In the light of above facts we synthesized a number of derivatives in order to increase the anti-inflammatory activity of cetirizine and, we did not perform antihistaminic activity of derivatives but more emphasis was laid on anti-inflammatory and immunomodulatory activities of these derivatives
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