Synthesis of 2-acetyl-substituted-1-naphthol was first carried out by the acetylation of substituted-1-napthol in presence of glacial acetic acid and zinc chloride. This compound on treatment with KCNS and Br2 yielded 2-(2-amino-1,3-thiazol-4-yl)-substituted-naphthalen-1-ol, which on facile condensation with aromatic aldehyde gave Schiff Bases. These on cyclo-condensation reaction with mercaptoacetic acid yields 4-thiazolidinone derivatives. The synthesized compounds were characterized by elemental analysis, 1H NMR, IR spectroscopy. Newly synthesized compound were also studied for their antimicrobial activities.