Synthesis, Pharmacological Activities, Structure-activity Relationship of 1,3,4-Oxadiazole-Piperazine Conjugates: A Review

Abstract

The conjugation of heterocyclic compounds often aims to leverage the beneficial properties of multiple compounds, which ultimately motivate the researchers to develop novel medicines with better efficacy, affinity, modified selectivity, dual/various modes of action, reduced side effects, lower cost, or enhanced therapeutic profiles. Hybrid molecules or conjugates for synergistic effect are obtained by combining structural features of two differently active fragments. Due to 1,3,4-oxadiazole’s alternating single and double bonds, each atom providing a porbital perpendicular to the molecule's plane is stabilized like a drug molecule. The conjugate of 1,3,4-oxadiazole with piperazine moiety exhibits a range of physiological effects such as lowering blood pressure, antimicrobial, antitubercular, antioxidant, anticancer, antiproliferative, etc. Numerous natural molecules with pharmacological importance have also been found to possess conjugation between piperazine and 1,3,4-oxadiazole. As there is a lack of studies that focused on the synthetic protocols, pharmacological potential, and structure-activity relationship of the conjugates of 1,3,4-oxadiazoles and piperazines, the presented article highlights specifically these dimensions which have been reported in the last 10 years (2014-2024) These details assist researchers in designing their studies, and it is hoped that researchers from various scientific fields will find the manuscript beneficial for their future work on the conjugates of 1,3,4-oxadiazoles and piperazine.