The process of drug discovery involves the identification, synthesis, characterization, screening, assay and development of new chemical entities that are suitable for medical and pharmaceutical use.2-thioxo-1, 2, 3, 4-tetrahydropyrimidine (THPM) are heterocyclic compound & represents are markable pharmacological efficient moieties and are with wide range of therapeutic properties.Synthetically they were synthesized using Multi-component reactions like Biginelli reaction or either microwave and conventional methods, having a multiple benefits of the time consuming and get high yield.In this review, we highlight recent developments on THPMs and recently developed as antimicrobial, anticancer, antiinflammatory, analgesic, antifungal, antibacterial, anti-tubercular, antihypertensive, analgesic, anticonvulsant, antioxidant, etc. given a potent biological and pharmacological activity.