Abstract 3-Substituted thieno [2, 3-d] pyrimidin-4 (3H)-one-2-mercaptoacetic acids and their ethyl esters were synthesized from 2-mercaptothieno [2, 3-d] pyrimidin-4 (3H)-ones, which were obtained by cyclization of thienylthioureas in acidic medium. Analgesic, anti- inflammatory, and anticonvulsant activities were found in some of these compounds. Significant antimicrobial activity was exhibited by thienylthioureas.