Alexander MacKerell
PHAR 531 - Pharmaceutical Chemistry Syllabus
Course Description
Modern pharmacy practice involves the dispensing of drugs and advice concerning their use. In order to properly advise patients on the use of drugs it is necessary to understand the mechanisms by which the drugs are absorbed and interact with their site of action. Such understanding is achieved by knowing how drug structure influences physical properties and their interactions with receptors. The Pharmaceutical Chemistry Course will present the conceptual background on these influences and provide essential prerequisite knowledge for the Medicinal Chemistry Course.
A variety of new drugs are coming to the market. Many of these new agents have compositions significantly different from traditional drugs (e.g. proteins versus small molecular weight organic compounds) and exploit novel biochemical mechanisms. In addition, the reemergence of natural products as pharmaceuticals raises issues concerning drug purity and variability. A pharmacist must be aware of these in order to optimize therapy and minimize adverse reactions.
As part of the Pharmaceutical Chemistry Curriculum, and consistent with the use of computers throughout the pharmaceutical industry, a computer lab is included. The computers lab is designed to reinforce the concepts being presented in the course, enhance problem solving abilities and encourage computer use in scholastic and professional endeavors.
Course Objectives
Upon completion of Pharmaceutical Chemistry students will have achieved 1) an overview of the relationship of drug structure to pharmacological activity, 2) an understanding of the processes involved in the design and development of modern pharmaceuticals and 3) an introduction to the cutting edge approaches that represent the future of pharmacy and 4) a suitable background for the Medicinal Chemistry Course.
Suggested Text
Williams, D.A. and Lemke, T.L., "Foye's Principles for Medicinal Chemistry: Fifth Edition, Lippincott, Williams & Wilkins, Baltimore, 2002. This text is not required, but it is the same text that will be used in Drug Chemistry and Medicinal Chemistry.
Handout Policy
All figures and lectures notes are available on the web, via this page. The links to the pages will be created when the final version of the notes are ready. Typically, PDF files are available for the complete lecture notes and for the overheads presented in the lecture, although this varies with instructor. This allows for the figures to printed for use during the lectures, while the complete notes may be downloaded onto your laptop to facilitate studying. It is suggested that students look at the lecture notes prior to class to facilitate following the lectures.
Prerequisites – Drug Chemistry, Biochemistry, Physical Chemistry
Instructors
Dr. Alex MacKerell, ADM
Dr. Ralph Blomster, RB
Dr. Andrew Coop, AC
Dr. Paul Shapiro, PS
Dr. Olgun Guvench, OG
All classes are in Room 120 at 10:00, unless noted.
Schedule
| Date | Topic | Instructor |
1/14 | HIV as a model of Rational Drug Design | ADM |
| 1/15 | HIV as a model of Rational Drug Design cont. | ADM |
| 1/16 | HIV as a model of Rational Drug Design cont. | ADM |
| 1/17 | Gene Therapy Cancer article siRNA article | PS |
| 1/18 | Introduction to Ligand-Receptor Model of Drug Action | ADM |
| 1/22 | Small Molecule SAR / Lead Compound Identification Powerpoint presentation | ADM |
| 1/23 | Lead Modification/Optimization Powerpoint presentation | ADM |
| 1/24 | Forces related to Drug Binding and Solvation | ADM |
| 1/25 | Role of aqueous solubility in drug binding/pKas Powerpoint presentation | ADM |
| 1/28 | Chiral Drugs Powerpoint presentation | ADM |
| 1/29 | Quantitative Structure-Activity Relationships QSAR Powerpoint presentation | ADM |
| 1/30 | Quantitative Structure-Activity Relationships cont. | ADM |
| 1/31 | Review session | |
| 2/1 | Exam 1, Lectures 1 through 10 (1/28 lecture) | |
| 2/4 | Quantitative Structure-Activity Relationships cont. | ADM |
| 2/5 | Lab 1 - Application of QSAR due 2/21, 10 am | ADM |
| 2/6 | Review of acid/base chemistry | AC |
| 2/7 | Role of acid/base chemistry in the solubility of drugs | AC |
| 2/8 | Role of acid/base chemistry to drug activity | AC |
| 2/11 | Drugs targeting DNA and RNA Powerpoint presentation | ADM |
| 2/12 | Enzyme Inhibition and Inactivation NOTE: Optional QSAR Lab Help Session, 12:00 to 1:50, 101 PH | ADM |
| 2/13 | Protein-protein Interactions as Drug Targets Powerpoint presentation | OG |
| 2/15 | RB | |
| 2/18 | Natural Products | RB |
| 2/19 | Top 20 Herbal Medicines | RB |
| 2/20 | Herbal Medicines: Toxicities, Side Effects, and Interactions | RB |
| 2/21 | Review/Discussion of Computer Lab 1 | ADM |
| 2/22 | Exam 2, Lectures 11 (1/29) through 21 (2/13) | |
| 2/25 | Pharmacogenomics Powerpoint presentation | ADM |
| 2/26 | Biotechnology-Based Drugs Powerpoint presentation | ADM |
| 2/27 | Biotechnology cont. | ADM |
| 2/28 | Biotechnoogy cont. | ADM |
| 2/29 | ADM | |
| 3/3 | Target Based cont. | ADM |
| 3/4 | Target Based Drug Discovery in Action | ADM |
| 3/5 | Dihydrofolate Reductase as a Paradigm Powerpoint presentation | ADM |
| 3/6 | Review Session | ADM |
| 3/7 | Final Exam, comprehensive with emphasis on material on lectures 22 | ADM |
For the Computer Help Sessions please bring your own computers. Attendance is optional.
Assessment
- Exams 85%
- Lab Project 15%
Grades will be 90-100% A; 80-89% B; 70-79% C; 60-69% D; <60% F.
Exam Policy
Three (3) exams will be given with the overall exam grade used to determine the final course grade the average of the three exams.
All exams will be initiated at the specified starting time. The exams, including scantrons, will be collected promptly at the specified finishing time. Individuals arriving late must still complete the exam by the specified finishing time. No individuals will be allowed to start the exam once another individual has completed the exam.
Individuals must inform the coursemaster of their inability to take an exam prior to the exam itself. The exam must then be taken within 36 hours of the starting time of the regularly scheduled exam. A note from a physician is required for an extension beyond this time limit. In all cases the makeup exam will include a 10 minute oral exam following completion of the written portion of the exam.
Past exams can be viewed here.
Computer Lab
The computer lab will be evaluated based on increments of 5%; i.e. 100%, 95%, 90%, 85%, 80%,,......0%. A 100% grade is based on a lab in which all requested data and plots are presented in a clear, concise and correct fashion and the text is well-written and addresses the requested and only the requested issues.
The computer lab is due promptly at the prescribed date and time. Due to that time corresponding with the presentation of results from the lab any lab handed in after that time will automatically lose points from those specified in the preceding paragraph. 10 pts will be lost on any lab handed in after the due date and time. Labs handed more than 12 hours after the due date and time will lose 20 pts and those handed in more than 2 days after the due date and time will lose 30 points.
Grading Policy
Grading of subjective portions of the the computer lab is designed to give the students the benefit of the doubt in all cases. Students are encouraged to discuss exam questions and computer labs with Dr. MacKerell or the appropriate instructor. Addition or any other accounting errors will be readily corrected.
Policy on Electronic Devices
The School of Pharmacy prohibits the use of individual electronic devices such as cell phones, personal data assistants (i.e., PDA's), programmable calculators, and portable computers during examinations. Exceptions to this policy are permitted when the use of one of more of these devices is integral to the evaluation process and explicitly authorized by the coursemaster.