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Pharmaceutical Chemistry 30:715:307 (2 credits) Fall 2018 Time: M, W 6:05-7:00 pm, PH-130 Course Description: The mission of the Pharmaceutical Chemistry course is to introduce students to the structure, properties, and analysis of pharmaceutical agents and metabolites as well as some fundamental techniques used for near patient testing and pharmacokinetic analysis. Topics include basic concepts in medicinal chemistry as well as methods of pharmaceutical and biomedical analysis: 1) the drug discovery and development process, 2) review of organic functional groups found in drug molecules, 3) drug-target interactions, 4) physicochemical properties related to drug action such as acid-base properties, equilibrium, and stereochemistry, 5) Chemistry of OTC inorganic drugs, 6) Effect of chemical structure on the metabolism of drug molecules, 7) Fundamentals of neurochemistry, and 8) Chromatographic (especially HPLC and LC-MS) analysis of pharmaceutical agents, metabolites, and clinical samples. Course Objectives: Students completing the Pharmaceutical Chemistry course will be expected to demonstrate the following abilities based outcomes (ABOs) 1. Develop and demonstrate depth and breadth of knowledge in biomedical, pharmaceutical, social/administrative/behavioral, and clinical sciences. (1.1.1) 2. Integrate knowledge from foundational sciences to explain how specific drugs or drug classes work and evaluate their potential value in individuals and populations. (1.1.2) 3. Apply knowledge in foundational sciences to solve therapeutic problems. (1.1.3) Course Instructors: Longqin Hu, Ph.D. (Coordinator) Professor of Medicinal Chemistry Email: longhu@pharmacy.rutgers.edu Allen N. Jones, Ph.D. Adjunct Professor, Medicinal Chemistry Email: allen.jones@rutgers.edu Michael Totleben, Ph.D. Adjunct Professor, Medicinal Chemistry Email: mt973@pharmacy.rutgers.edu Course Material: Textbook, Study Guide, and Class Lectures https://sakai.rutgers.edu/ Required Textbook: Organic Chemistry Concepts and Applications for Medicinal Chemistry, Joseph E. Rice, Academic Press, 2014, Softcover; ISBN 9780128007396 or eBook; ISBN 9780128008324. Reference Books: David G. Watson. Pharmaceutical Analysis, A Textbook for Pharmacy Students and Pharmaceutical Chemists, 3rd Edition, 2012, Elsevier. Examinations: Three exams (two mid-terms and one comprehensive final) and around 10 in-class quizzes. The final is optional for students w/ average 70 after the second mid-term exam. Grading: Exam 1 25% Exam 2 25% Quizzes 15% Final Examination (cumulative) 35% Total 100% Pharmaceutical Chemistry 30:715:307 Fall 2018 Pharmaceutical Chemistry Fall 2018 Tentative Course Outline: Week Lecture Topics covered Course Introduction and Importance of Pharmaceutical Chemistry in Understanding Drug Action and Clinical Test Results (Hu): Drug 1 Lecture 1 discovery and development process, Sequence of events after drug administration, List of physico-chemical properties related to drug action, Clinical Chemistry and the importance of fundamental chemistry concepts and analytical techniques Lecture 2 Review of Organic Functional Groups and Acid-Base Concepts 2 (Totleben): Chemical bonding Lecture 3 Lecture 4 Drug-Target Interactions (Hu): Structural Effects on Biological Action, 3 Role and types of chemical bonding interactions between drug and target, Lecture 5 Binding of neurotransmitters to their receptors, Thalidomide: Lessons as related to chirality of drugs Lecture 6 4 Review of Organic Functional Groups and Acid-Base Concepts Lecture 7 (Totleben): Functional groups, Electron donating and withdrawing Lecture 8 groups; Acids and bases, Henderson-Hasselbach equation; Estimating pK and pK ; Heterocycles 5 a b Lecture 9 Lecture 10 Review of Stereochemistry and Physico-Chemical Properties Related to 6 Drug Action (Totleben): Stereoisomers, Stereochemistry of unsaturated Lecture 11 compounds, Enantiomers, Diastereomers, Partition coefficients Chemistry of Over-the-Counter (OTC) Inorganic Drugs (Hu): Structures, ® Lecture 12 chemical properties and mechanisms of action of antacids (Tums , Pepto- 7 Bismol, Milk of Magnesia), inorganic germicides, imaging agents, and platinum anticancer agents Lecture 13 Fundamentals of Neurochemistry (Hu): Structures, chemical properties, metabolism, and actions of select neurochemicals including acetylcholine, Lecture 14 epinephrine, norepinephrine, dopamine, serotonin, glutamate, GABA, and nitric 8 oxide) and of nicotine Exam 1 Midterm Exam 1 (cover lectures 1-13) Pharmaceutical Chemistry 30:715:307 Fall 2018 Lecture 15 Fundamentals of Neurochemistry (Hu): (Cont’d) 9 Chemical Aspects of Drug Metabolism (Hu): Introduction, Effects of Lecture 16 chemical structure on Phase I oxidative, reductive, and hydrolytic reactions, Lecture 17 Effects of chemical structure on phase II conjugative reactions (COMT and PNMT-catalyzed methylation, acetylation, sulfation, glucuronidation, amino 10 acid conjugation, mercapturic acid formation), Sites of metabolism, Metabolic Lecture 18 pathways of selected common drugs, Metabolites identified for a new anticancer drug, Imatinib Lecture 19 Introduction to Analytical Separations (Jones): Basic separation techniques 11 in chemistry laboratories and in clinical drug monitoring, Extraction, Effect of Lecture 20 pH, Available formats and types of chromatographic techniques, Efficiency of Lecture 21 separation, van Deemter equation 12 Thanksgiving Recess Lecture 22 13 Chromatographic Analysis of Pharmaceutical Agents, Metabolites, and Lecture 23 Clinical Samples (Jones): HPLC components, Separation process in comparison with GC, Classification based on retention mechanisms, Normal vs Lecture 24 reversed phases, Isocratic vs gradient elution, Criteria of good separation, 14 Applications of HPLC in quantitative analysis of pharmaceutical agents and Lecture 25 metabolites, Hyphenated techniques in clinical drug monitoring, LC-MS in the metabolism and disposition studies of drugs – metabolite patterns in patients urine, plasma Lecture 26 15 Exam 2 Midterm Exam 2 (covering lectures 14-26) 16 Finals Comprehensive Final Exam (optional for students w/ 70%) Week Required Textbook: Organic Chemistry Concepts and Applications for Medicinal Chemistry, Joseph E. Rice, Academic Press, 2014, Softcover; ISBN 9780128007396 or eBook; ISBN 9780128008324. Reference Book: David G. Watson. Pharmaceutical Analysis, A Textbook for Pharmacy Students and Pharmaceutical Chemists, 3rd Edition, 2012, Elsevier. https://sakai.rutgers.edu/
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