Synthesis and Biological Evaluation of 3-(Methoxymethyl) Pyrazole Analogues as Antagonists for Dopamine Receptors

초록

The exploratory search of new ligands with high binding affinity and good selectivity for the dopamine D4 receptor is an main concern for the development of new antipsychotic therapeutics in treating schizophrenia. However, classical dopamine D2 antagonist like haloperidol has a severe side effect such as extrapyramidal one resulted from the blockage of D2 receptors in the striatum of brain. In this study, we designed and synthesized new 3-(methoxymethyl) pyrazole analogues coupled with the phenyl piperazine system for the discovery of new antipsychotic compound. The biological activity of a synthesized small 3-(methoxymethyl) pyrazole library will be discussed.