An Overview of Piperazine Scaffold as Promising Nucleus for Different Therapeutic Targets

Abstract

: Piperazine scaffolds are a group of heterocyclic atoms having pharmacological values and shows significant results in pharmaceutical chemistry. Piperazine has the flexible core structure for the design and synthesis of new bioactive compounds. These flexible heterogenous compounds exhibit various biological roles, primarily anticancer, antioxidant, cognition enhancers, antimicrobial, antibacterial, antiviral, antifungal, anti-inflammatory, anti-HIV-1 inhibitors, antidiabetic, antimalarial, antidepressant, antianxiety and anticonvulsant activities etc. In the past few years, researchers focused on the therapeutic profile of piperazine synthons for different biological targets. The present review highlights the development in designing and pharmacological activities of nitrogen-containing piperazine moiety as a therapeutic agent. The extensive popularity of piperazine as a drug of abuse and their vast heterogeneity research efforts over the last years motivated the new investigators to further explore this area.

Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

“…More generally, the recent C-H functionalization methods of the piperazine ring should be compared and contrasted with the pioneering examples of CH-piperazine functionalization, including Rh, Ta, and Cu catalysis [36][37][38]. The reader is further encouraged to consult additional reviews on the topic of the synthesis and application of piperazines [39][40][41].…”

Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities

“…In vitro agonistic activities on MT 1 and MT 2 receptors via the Tango GPCR assay. Considering that the piperazine framework was a valuable pharmacophore for many drugs for the treatment of central nervous system diseases, 21 the most active compound 18 with a piperazine fragment was selected for further research. To confirm the agonistic activity of compound 18 on MT 1 and MT 2 receptors, we performed a Tango GPCR assay.…”

Piperazine, a Key Substructure for Antidepressants: Its Role in Developments and Structure‐Activity Relationships

“…Although there are some reports published on ongoing developments of piperazine‐based therapeutic targets [18,19,23,47–49] . the current work provides critical understanding of the role of piperazine scaffold in the current work on antidepressants (2015 onwards) along with their SAR studies.…”