Construction and Binding affinity of n-Butyl Pyrazole Library as Antagonist of D4 receptor

초록

The malfunction of central nervous system is well known to be the cause of mental disorder for a long time. Recently, it is well known that dopamine D4 receptors in mental disorder such as schizophrenia or attention deficit hyperactivity disorder [ADHD] had to be involved. In this study, the n-butylpyrazole heterocyclic library coupled with the phenyl piperazine derivatives were designed as the promising candidate molecular structure on the selective dopamine D4 receptor antagonist. From the well established synthetic pathway, a library of 52 compounds was synthesized and evaluated for their biological activity in vitro. The screening results of a few selected compounds on the dopamine D4 receptor were shown the excellent IC50 value under 10 nM scales.