The field of medicinal chemistry is an exciting and dynamic area of study that has played a crucial role in the development of modern medicine. Medicinal chemistry is a multidisciplinary science that integrates principles of chemistry, biology, and pharmacology to design, develop, and optimize small molecules for therapeutic use. The Pharmacy Council of India (PCI) recognizes the importance of medicinal chemistry in pharmacy education and has included it in the B. Pharm &Pharm.Dcurriculum. The aim of the medicinal chemistry course is to provide students with a comprehensive understanding of the principles of drug design and development, the structure-activity relationships of drugs, and the mechanisms of drug action. This lab manual on medicinal chemistry has been designed to complement the PCI syllabus and provide students with hands-on experience in drug design, synthesis, and characterization. The manual includes a series of experiments that cover different aspects of medicinal chemistry, such as drug design and optimization, drug synthesis, and drug characterization. The experiments have been carefully selected to provide students with a broad understanding of the principles and techniques used in medicinal chemistry. Each experiment is accompanied by clear instructions, background information, and safety guidelines to ensure that students can carry out the experiments safely and effectively. We hope that this lab manual will serve as a valuable resource for students and teachers alike and will contribute to the development of skilled professionals in the field of medicinal chemistry. We would like to thank the Pharmacy Council of India for recognizing the importance of medicinal chemistry in pharmacy education and for providing students with the opportunity to study this fascinating field.We believe that the practical knowledge gained through these experiments will help students to develop a deeper understanding of medicinal chemistry and prepare them for successful careers in the pharmaceutical industry.