Schizophrenia is a chronic neuropsychiatric disorder that affects nearly 1% of the global population. There are various anti-psychotic drugs available for the treatment of schizophrenia, but they have certain side effects; therefore, there is a need to explore and develop novel potential lead compounds against schizophrenia. The currently available drugs e.g. typical and atypical antipsychotics act on different dopamine and serotonin receptors and as per literature reports, various piperidine and piperazine derivatives have shown promising activity against these receptors. When different heterocyclic groups are attached to basic piperidine and piperazine rings, the antipsychotic activity is greatly potentiated. In this direction, various antipsychotic drugs have been synthesized at the laboratory level, and few are under clinical trial studies, such as Lu AE58054, PF-04802540, ORG25935, DMXB-A, Bitopertin, and ABT-126. In the present review, we include the studies related to the effect of different substituents on piperidine/piperazine derivatives and their anti-psychotic activity. Various series of synthesized compounds by other researchers with piperidine/piperazine nucleus have been reviewed and diagrammatically represented in the form of SAR (structure-activity relationships), which will help the scientists for the development of potential lead compounds.

精神分裂症是一种慢性神经精神病，影响全球近1％的人口。有多种抗精神病药可用于治疗精神分裂症，但它们有一定的副作用。因此，有必要探索和开发新型抗精神分裂症的潜在先导化合物。当前可获得的药物，例如典型的和非典型的抗精神病药，作用于不同的多巴胺和5-羟色胺受体，并且根据文献报道，各种哌啶和哌嗪衍生物已显示出针对这些受体的有希望的活性。当不同的杂环基团连接到碱性哌啶环和哌嗪环上时，抗精神病活性将大大增强。在这个方向上，已经在实验室水平上合成了多种抗精神病药物，并且很少进行临床试验研究，例如Lu AE58054，PF-04802540，ORG25935，DMXB-A，Bitopertin和ABT-126。在本综述中，我们包括与不同取代基对哌啶/哌嗪衍生物的作用及其抗精神病活性有关的研究。其他研究人员利用哌啶/哌嗪核合成了各种系列的化合物，并以SAR（结构-活性关系）的形式进行了图解说明，这将有助于科学家开发潜在的先导化合物。