BACKGROUND Tuberculosis (TB) is an acute or chronic infectious disease caused by several species of Mycobacterium, collectively called tubercle bacilli or Mycobacterium tuberculosis complex. Around 10 million people get sick with tuberculosis (TB) each year. TB is the second leading cause of death today after HIV/AIDS. A serious problem in the context of MDR-TB is the extensively drug-resistant TB, which is an important reason for the restricted chemotherapy in TB. Therefore, there is a need to explore new antitubercular (anti-TB) agents. Coumarin is an oxygencontaining heterocyclic compound and can be widely found in many natural products, and many of them display diverse biological activities. The wide spectrum of activities of coumarin molecules has intrigued the scientists to explore the natural coumarins and their synthetic derivatives for their potential as anti-TB drugs. OBJECTIVE The objective of this review is to emphasize important coumarin analogs with anti-TB activities and their structure-activity relationships (SAR) for designing better anti-TB agents. METHODS Latest, authentic and published reports on various synthetic and natural coumarin derivatives and their anti-TB activities is being thoroughly studied and analyzed. The structural requirements of coumarins as anti-TB drugs have also been studied. RESULTS Collection and compilation of reports on various synthetic and natural coumarin derivatives and their anti-TB activities are being performed. CONCLUSIONS The study provides the latest report on coumarin derivatives synthesized as anti-TB agent and whether their activity depends on structural changes or not.