Medicinal chemistry has been developed carefully and expanded meticulously according to the latest PCI–approved syllabus meant for the pharmacy degree programmes (B. Pharm) in all Indian universities and others abroad offering similar curricula. The entire textual matter runs over five units comprising seventeen chapters that may certainly prove to be of good readability, immense utility, and brilliant adaptability not only confined to B. Pharm aspirants but also to various M. Sc. (Chemistry) courses as well. Salient features include concise and lucid presentation of scientific information. Detailed skill related to drug design–synthesis to acquire a better knowledge in medicinal chemistry. Special emphasis on chemical nomenclature, synthesis of drugs, their explanations, uses. Presented in a unique, simple and informal style so as to enable the UG/PG students to have a better clarity of fundamental ideas and concepts in medicinal chemistry. Each Chapter is provided with review questions and further selected references to help the brilliant students to grasp the subject in a better manner perceptively.