In present day scenario, tetrazole has gained increasing popularity due to its broad-spectrum of biological properties such as antitubercular, anticancer, antimalarial, antidiabetic, antifungal, anti-inflammatory activities etc. Tetrazole, beinga bioisostere of the carboxylic acid group can replace the carboxyl group in drugswhich can be utilized to increase the lipophilicity, bioavailability and to reduce theside effects of drugs. Many tetrazole containing compounds have already been used for the treatment of various diseases primarily due to their better pharmacokineticprofile and metabolic stability. Therefore, this heterocyclic tetrazole moiety having admirable biological, pharmaceutical and clinical applications can be considered as an important pharmacophore in the development of new drugs.The presentsurveyreviews the various approaches available for the synthesis of tetrazole derivatives along with the different biological activity of substituted tetrazole derivatives like antitubercular, anticancer, antimalarial, antidiabetic, and antifungal and anti-inflammatory. This survey will serve as a comprehensive database of the biological, pharmaceutical and clinical applications of tetrazole which will be beneficial in facilitating further research and development on the topic.