Tetrazoles: Synthesis and Biological Activity

Author(s): Niranjan Kaushik*, Nitin Kumar, Anoop Kumar, Umesh K. Singh

Journal Name: Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Under Re-organization)
Formerly Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents

Volume 18 , Issue 1 , 2018

Graphical Abstract:


Background: In present decades, interest in tetrazole chemistry has been increasing rapidly because of its broad range of biological applications, primarily due to the role played by tetrazole in medicinal chemistry as this moiety offer a more complimentary pharmacokinetic profile and a metabolically stable substitute for carboxylic acid functionalities. The heterocyclic tetrazole moiety has admirable biological, pharmaceutical and clinical applications.

Method: There are various approaches available for the synthesis of tetrazole derivatives which are reported in the present survey. The most versatile method for the synthesis of tetrazoles is [2+3] cycloaddition reaction between nitriles and azides.

Observations: Among the family of nitrogen-containing heterocycles, tetrazole and its derivatives exhibit a large range of biological properties such as antibacterial, antifungal, anticancer, analgesic, anti-inflammatory, antidiabetic, anti-hyperlipidemic and antitubercular activities. The unique features of tetrazole, biological significance and applications are discussed in this review.

Conclusion: The present investigation reviews the various synthetic approaches and different biological activity of substituted tetrazole derivatives. The rationale of this review was to pool literature work reported by researchers on tetrazole for their various biological activities and also reported current efforts made on tetrazole moiety.

Keywords: Tetrazole, synthesis, anti-inflammatory, anti-diabetic, anticancer, antibacterial activity.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2018
Published on: 05 September, 2018
Page: [3 - 21]
Pages: 19
DOI: 10.2174/1871522218666180525100850
Price: $65

Article Metrics

PDF: 318