In the drug design involves the synthesis of small molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it. Although extensive research has been performed on medicinal chemistry or drug design for many years, there is still deep need of understanding the interactions of drug candidates with biomolecules. This book entitled "The textbook of Enzyme inhibition and Medicinal Chemistry" contains a selection of chapters focused on the research area of enzyme inhibitors, molecular aspects of drug metabolism, organic synthesis, pro-drug synthesis, in vivo studies and chemical compounds used in relevant approaches.