An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review

Piperazine, is privileged six membered nitrogen containing heterocyclic ring also known as 1,4-Diazacyclohexane. Consequently, piperazine is a versatile medicinally important scaffold and is an essential core in numerous marketed drugs with diverse pharmacological activities. In recent years several potent molecules containing piperazine as an essential subunit of the structural frame have been reported, especially against Mycobacterium tuberculosis (MTB). Remarkably, a good number of these reported molecules also displayed potential activity against multidrug-resistant (MDR), and extremely drug-resistant (XDR) strains of MTB. In this review, we have made a concerted effort to retrace anti-mycobacterial compounds for the past five decades (1971-2019) specifically where piperazine has been used as a vital building block. This review will benefit medicinal chemists as it elaborates on the design, rationale and structure-activity relationship (SAR) of the reported potent piperazine based anti-TB molecules, which in turn will assist them in addressing the gaps, exploiting the reported strategies and developing safer, selective, and cost-effective anti-mycobacterial agents. (C) 2020 Elsevier Masson SAS. All rights reserved.

Automated summary

Piperazine, a nitrogen-containing heterocyclic compound, is widely used in medicinal chemistry for its diverse pharmacological activities, particularly in the development of anti-TB molecules. Studies have shown that molecules containing piperazine subunits exhibit potential activity against drug-resistant strains of Mycobacterium tuberculosis.