Indeed, the scaffold of thiazolidin-4-one (4-oxo-thiazolidine) has garnered significant interest in the medicinal chemistry due to its versatility and diverse biological activities, including potential applications in anti-tuberculosis (anti-TB) drug discovery. Its structural properties enable modifications, facilitating the development of various small molecules with desirable pharmacological properties. The review outlines the various medical uses, (anti-TB properties), of thiazolidin-4-derived compounds over the past two decades, highlighting promising candidates such as 53a, 53b, and 53d, which have demonstrated MICs (0.05-0.2) μg/ml against the strain of M. TB H37Rv, along with compound 108 exhibiting a MIC of 0.36 mM. Additionally, compounds 55b, 56, 54k and 54i have shown full effectiveness against Mycobacterium TB (H37Ra), with MIC (0.031-0.125) μg/ml. Acidomycin has exhibited high activity against MDR and XDR as a various strains. This review also explores SAR of the tested compounds and their potential targets.