藥物化學

Instructor: Professor Jacquelyn Gervay-Hague jgervayhague@ucdavis.edu Office Hours: Please schedule an appointment here: https://calendly.com/jgervayhague/30min Course Description: This is a three-week accelerated course that provides an introduction to the bioorganic chemistry principles behind the design and production of pharmaceutical agents. The course content is focused on explaining and predicting how small organic molecules bind to biological receptors, inhibit enzymes, and are metabolized. This course will draw on and expand upon material covered in introductory organic chemistry such as proposing reasonable arrow-pushing mechanisms for organic reactions and predicting the reactivity of organic molecules with particular reagents. Schedule: 09:00-12:00 on 3/31, 4/2, 4/7, 4/9, 4/14, 4/16 Venue: R208, IBC, AS Outline of Lecture Topics Topic 1: Basic Organic Chemistry Principles and the Drug Discovery Process Concepts to be covered - Basic Organic Chemistry Mechanisms Natural products Drug Discovery Clinical Trials Enzyme structure Lead compounds Pharmacophore Lead modification Prodrug Bioavailability and biodistribution Rule of five Topic 2: Antivirals Concepts to be covered - Viral protein targets SAR to achieve Enzyme inhibition Competitive inhibition Small molecule prophylactic Drug/protein interactions Viral replication Structure of RNA Mechanism of Action Vaccines: Immune response Antibody-based formulations Topic 3: Antibiotics and Anti-inflammatories Concepts to be covered - Bacterial replication Resistance Compliance Enzyme inactivation, prodrugs COX inhibition NSAIDS Topic 4: Anticancer Therapies Concepts to be covered - ADME Routes of Administration Absorption BBB Topic 5: Progress in Addiction Medicine

Policies: Strategies for success: Attend all in-class lectures, take detailed notes, which should be primary study source. Quiz material will almost entirely come from the class notes. Group study is highly recommended. The group can compare class notes and help each other understand the material. Regrades: Legitimate questions about the grading of quizzes (either the grading of a particular problem or an addition error in the score) can be submitted up to one day after the quiz is handed back. The procedure for submitting a regrade request is to attach a separate piece of paper to the front of the quiz with the question(s) to be regraded and a brief justification for the regrade. Do not write on the quiz itself or it may not be accepted for a regrade. UC Code of Conduct policies will be enforced: https://ossja.ucdavis.edu/code-academic-conduct

Course Grading: Attendance 20% Quizzes 60% Final Design Project 20% Attendance & Participation: Full credits are given for those who attend all lectures punctually and participate actively when called on during lecture. Quizzes: There are 3 Take Home Quizes - Quiz 1 covers lectures 1 and 2; Quiz 2 covers lectures 3 and 4; Quiz 3 covers lectures 5 and 6. You may use your notes and the textbook, and you may work with your classmates on the quizzes, however you must turn in your own work in hard copy by 5 pm on the specified deadline. Design Project: Weekly design labs will be dedicated to individual projects to design a therapeutic drug.

"The Organic Chemistry of Drug Design and Drug Action, 3rd Edition" Richard B. Silverman and Mark W. Holladay Chemistry 130A will cover parts of Chapters 1 through 6. Assigned reading pages and end of Chapter homework problems (in parenthesis): Readings Chapter 1: 1-15; Homework (1-6) Readings Chapter 2: 17-35, 54-83; Homework(8-10, 24-26) Readings Chapter 3: 123-157; Homework(1, 3, 4, 7) Readings Chapter 4: 165-195; Homework(1, 4, 6, 7, 10a, 11, 12, 14) Readings Chapter 5: 208-256; Homework(1, 2, 4, 6, 8, 14a) Readings Chapter 6:275-318; Homework(2, 3, 6, 7, 11, 15)