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.