Tuberculosis (TB), mainly caused by Mycobacterium tuberculosis, is the leading killer among all infectious diseases worldwide
and is responsible for more than two million deaths annually. The recent increase in the number of multi-drug resistant clinical isolates
of M. tuberculosis has created an urgent need for the discovery and development of new antituberculosis leads. This review covers
recent reports terpenoids that have demonstrated moderate to high activity in bioassays realized in vitro against M. tuberculosis; their organic
synthesis is included in some cases. In this review, monoterpenoids, diterpenoids, sesquiterpenes, sesterterpenes and triterpenes,
their structural analogs and semisynthetic derivatives will be discussed, with particular emphasis on the reported syntheses for each compound.