The role of thiophene and thiazolidinone derivatives in drug design and synthesis of pharmacologically important molecules has grown enormously worldwide. These systems are widely used in organic chemistry as intermediate for the synthesis of numerous compounds and these compounds possess remarkable biological activities. These scaffolds have been consistently rewarded as a promising versatile lead molecule with a pivotal position in modern medicinal chemistry. A major aim of this book was to provide recent literature regarding the Importance of Thiophene/Thiazolidinone derivatives in the medicinal chemistry.