1. Why Should I Take This Course?

Have you ever wondered how aspirin reduces inflammation and relieves pain, or how Gleevec precisely targets cancer cells? These life-saving medications are not accidental discoveries—they are the result of rational design by medicinal chemists. If you are curious about the following, this course is for you:

• Driven by curiosity: Eager to understand how drugs act like a "lock and key" inside the human body.
• Career-oriented: Aspiring to become a scientist in drug discovery, a pharmaceutical analyst, a regulatory expert, or a clinical researcher.
• Future-ready: Seeking core competencies in the promising field of biomedicine.

Learning medicinal chemistry will allow you to not only know what a drug treats but also why it works—a crucial step in transforming from a knowledge consumer to a knowledge creator.

2. What Is This Course About?

The core theme of this course is "Drug Discovery and Optimization." We will systematically explore how to progress from a biological target (such as a key protein) to designing, optimizing, and ultimately obtaining a safe and effective clinical drug candidate.

Specifically, we will delve into three key modules:

• Fundamental Principles: Learn about the journey of drugs in the body (ADME) and the core chemical principles of drug-target interactions.
• Design Strategies: Explore modern drug design methods, such as analyzing structure-activity relationships, applying bioisosterism for molecular optimization, and designing prodrugs to improve drug properties.
• Real-World Case Studies: Examine the complete development process of classic drugs (e.g., antihypertensives, antibiotics) to understand how theory is applied in practice.

3. What Will You Gain from This Course?

• A Systematic Knowledge Framework: Acquire a comprehensive understanding of the entire drug discovery process and how chemistry, biology, and pharmacology collaborate.
• Cutting-Edge Thinking Tools: Learn to think like a medicinal chemist, mastering rational design approaches such as structure-based and property-based drug design.
• Enhanced Problem-Solving Skills: Through case studies and projects, develop the ability to balance multiple factors like efficacy, safety, and pharmacokinetics.
• Improved Career Competitiveness: Whether you pursue R&D, production, regulation, or investment, the knowledge gained here will set you apart.

4. What Makes This Course Unique?

• Integration of Classic and Cutting-Edge Content: Covers established medicinal chemistry principles while introducing advanced technologies like computer-aided drug design and PROTACs.
• Case-Driven Teaching Approach: Focuses on real-world problems rather than isolated知识点, using success and failure stories from actual drug development to make abstract concepts tangible.
• Interdisciplinary Perspective: Emphasizes the integration of chemistry, biology, and medicine to cultivate a holistic view essential for modern drug discovery.
• Transferable Skill Development: The rational design thinking and analytical skills taught are applicable to other scientific fields and even complex business challenges.

To enable students to systematically master the core principles and fundamental methods of modern drug discovery, cultivate their preliminary ability for rational design and analysis of drug molecules, and establish a solid theoretical foundation and practical skills for their future advanced studies, research and development, or career development in fields related to pharmaceuticals, chemistry, and biomedicine.

To help you successfully learn and thoroughly master the content of the Medicinal Chemistry course, we strongly recommend having a foundational knowledge in the following subjects before the course begins. This knowledge serves as the cornerstone for understanding drug molecule design, mechanisms of action, and optimization strategies: (1) Core Prerequisites: Organic Chemistry, Biochemistry, Human Anatomy and Physiology. (2) Important Supplementary Knowledge: Pharmacology, Analytical Chemistry

I. Core Textbooks

These books establish the systematic knowledge framework of medicinal chemistry and form the foundation of course learning.

1. An Introduction to Medicinal Chemistry by Graham L. Patrick

• Features: One of the most popular introductory textbooks worldwide. Known for its clear language, thorough explanations, and rich illustrations, making it highly suitable for beginners. Each chapter uses specific drug examples to illustrate theoretical concepts, facilitating understanding.
• Application: Recommended as the primary supporting textbook for the course.

1. The Practice of Medicinal Chemistry edited by Camille G. Wermuth, et al.

• Features: Emphasis on "practice," offering in-depth exploration of strategies, methods, and challenges in drug design and optimization. Regarded as the "bible" for medicinal chemists. More advanced than Patrick’s text, suitable for further study after mastering the basics.
• Application: An essential reference for motivated students, graduate students, and future R&D professionals.

1. Foye's Principles of Medicinal Chemistry by David A. Williams, et al.

• Features: A classic comprehensive work, systematically organized by disease and therapeutic areas (e.g., nervous system drugs, cardiovascular drugs). Provides detailed pharmacological and chemical insights into each drug class.
• Application: Serves as an authoritative desk reference for detailed information on specific drug categories.

II. Case Studies & Drug History

These resources present knowledge through storytelling, making theoretical content engaging and cultivating scientific thinking.

1. The Billion-Dollar Molecule: One Company's Quest for the Perfect Drug by Barry Werth

• Features: A nonfiction work vividly depicting Vertex Pharmaceuticals’ early challenges in developing an FK506 analog immunosuppressant. Offers deep insight into the real world of drug development—interweaving science, business, human factors, and luck.
• Application: Ideal for extracurricular reading to spark interest and understand the broader context of drug R&D.

1. The Drug Hunters: The Improbable Quest to Discover New Medicines by Donald R. Kirsch

• Features: Traces the history of drug discovery from ancient times to the modern era, filled with fascinating anecdotes and cases. Highly readable.
• Application: A relaxed and enjoyable introductory read to understand the evolution of drug discovery.

III. Online Databases & Tools

These are essential "digital laboratories" for modern medicinal chemists.

1. PubChem

• URL: https://pubchem.ncbi.nlm.nih.gov/
• Description: A free chemical database maintained by the NIH. Allows queries of chemical structures, physical properties, biological activities, toxicity, and related literature for nearly all small molecules. Essential for assignments and literature research.

1. Protein Data Bank (PDB)

• URL: https://www.rcsb.org/
• Description: A repository of 3D structures of biological macromolecules (e.g., proteins, DNA/RNA). Enables visualization of precise binding modes between drugs and target proteins, illustrating the "lock and key" relationship.

1. DrugBank

• URL: https://go.drugbank.com/
• Description: A unique bioinformatics and chemoinformatics resource integrating detailed drug data (chemical, pharmacological, pharmaceutical) with target information (sequence, structure, pathways). Ideal for comprehensive searches on marketed drugs.

IV. Professional Journals

For tracking cutting-edge advances; suitable for advanced students or those undertaking graduation projects.

• Journal of Medicinal Chemistry: A top-tier journal in the field, representing the highest industry standards.
• ACS Medicinal Chemistry Letters: Publishes concise, novel research communications.
• Nature Reviews Drug Discovery: Features authoritative reviews summarizing and forecasting trends in specific areas—the best source for quickly grasping hot topics.