Tuberculosis (TB) is a serious, life‐threatening infectious disease that mostly affects the lungs and is caused by Mycobacterium tuberculosis (MTB). Still, in 2024, because of its widespreadness, contagious nature, and an increasing number of patients with other diseases, it is hard to cure, and leftovers as the deadliest disease to mankind across the world. In recent years, abundant efforts have been made to cure and eradicate TB, but drug‐resistant TB (DR‐TB) or multidrug‐resistant TB (MDR‐TB) surges the rate of mortality. Recently, World Health Organization (WHO) released the Global Tuberculosis (TB) Report 2022, in which the millions of infections and deaths stretched a line of serious concern to the scientists. In pursuit of searching for novel anti‐TB agents, several derivatives of sulfonamides have been synthesized and tested for their anti‐TB activity. It is noteworthy that lead compounds contain sulfonamide functionalities, which are the privileged motifs that act as crucial pharmacophores in many bioactive compounds and have diverse biological activities, including analgesics, antitubercular, antifungal, antidepressant, anti‐inflammatory, antihypertensive, antidiabetic, anticancer, antimalarial, antioxidant, antimicrobial, etc. The review encapsulates the latest methods for preparing sulfonamide derivatives and their groundbreaking medicinal applications from 2007 to 2020.