Synthesis And Antiallergic Activity Of I-diphenylmethyl Piperazine Derivatives

The allergy disease is very common. Among the therapies for it, histamineH₁ receptor antagonists (antihistamines) are used effectively for treating thisdisease non-specifically. With the disease rising increasingly at the present time,the study and exploiture on the newer antihistamine that has more significanteffect and less side-effect has been paid more attention by researchers.Through investigating many antihistaminic drugs of piperazines, thestructure of 1-diphenylmethyl piperazine should be an essentially active part.Based on the fact, eleven target compounds of 1-diphenylmethyl piperazines(formula was followed) were designed with structure modification. The targetcompounds could be divided into tow species: non-substituent and substituent1-diphenylmethyl piperazine.The target compounds were synthesized with reasonable synthetical way,and were identified by MS, IR, ¹H-NMR and elemental analysis. The regular oftheir MA, IR, ¹H-NMR data were summarized furthermore. In addition, themelting points of them were measured with B-type tube.The activities of target compounds were evaluated in the antihistanimicexperiment. The results showed that all of them had some effects. Among them,wj01, wj02, wj07 and wj08 had more significant effect than the control group(P＜0.05). But their effects were inferior to that of the chlorpheniramine.