Abstract
Pyrimidine and piperazine are well known as being the backbone of many bulky compounds and a vital core structure in approved drugs; previous studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity. Despite vast resources enriched with a heterocyclic hybrid structure, a few reported studied on the synthesis and biological activities of pyrimidine-piperazine analogs were discussed. In this review, we summarize current design methods for the construction of pyrimidine-piperazine hybrids by coupling substituted piperazine on various positions of a pyrimidine ring and studied their biological studies.