The contents of this course have been scrupulous designed to provide understanding of the basic biological and pharmacological interactions by using both natural products and total synthesis of bioactive molecules. It will also be useful to the graduate students studying modern methods knowledge in tactics and strategies for synthesis in medicinal chemistry. It will be helpful for the use of corresponding knowledge for the development of biologically and clinically active drugs. It will include advanced courses in natural products, organic synthesis, medicinal chemistry; fundamentals of cell biology, molecular biology, drug design. Particular emphasis has been laid on the pharmaceutical substances that are specially found in the Official Compendia. It will also be involved to demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics and the role of medicinal chemistry in improving these parameters. It will be helpful in relating the structure and physical properties of drugs to their pharmacological activity as well as describe the current challenges and opportunities in medicinal chemistry in light of contemporary developments in the field of drug discovery. It will also cater to scientists and investigators, working in other fields of pharmaceutical sciences who wish to update their personal wealth of knowledge and understanding of the intricacies of modern methods of Medicinal Chemistry.