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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Mini-Review Article

Synthetic Protocols, Structural Activity Relationship, and Biological Activity of Piperazine and its Derivatives

Author(s): Md Faizan, Rajnish Kumar*, Avijit Mazumder, Salahuddin, Neelima Kukreti, Arvind Kumar and M.V.N.L. Chaitanya

Volume 20, Issue 8, 2024

Published on: 29 April, 2024

Page: [753 - 780] Pages: 28

DOI: 10.2174/0115734064304396240415110015

Price: $65

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Abstract

The versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six-membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability, and ADME characteristics, as well as improved target affinity and specificity. Various synthetic protocols have been reported for piperazine and its derivatives. In this review, we focused on recently published synthetic protocols for the synthesis of the piperazine and its derivatives. The structure-activity relationship concerning different biological activities of various piperazine-containing drugs was also highlighted to provide a good understanding to researchers for future research on piperazines.

Keywords: Piperazine, pharmacological activity, structural rigidity, bioavailability, affinity, specificity, structure-activity relationship.

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