Currently, schizophrenia, as a serious psychiatric disorder, continues affecting the quality of life in the psychotics.
This disease is often debilitating and chronic, showing broad symptoms at one end by hallucinations, delusions,
thought disorder and the other end by affective flattening, catatonia, social isolation. In order to combat this disease, many
antipsychotic drugs have been developed and introduced into clinical practice in the past half century. However, only a
small minority of them can treat effectively schizophrenia without side effects. In view of this situation, high attention has
been given to the exploration of desired antipsychotic agents influential especially through the modulation of dopamine
and serotonin receptors with substantial strides made in recent years, leading to the discovery of many novel chemical entities
with intriguing profiles. In this review, we summarize novel structural antipsychotics in development and discuss the
future direction of ideal antipsychotic drug candiates. In particular, the promising atypical antipsychotic profiles of new
molecules and the inspirations for their design are highlighted.