Fundamental medicinal chemistry 7-S3-5-CH-W-D1
A. Lecture and seminar
History of medicinal chemistry. Classification of medicines. Drug targets (enzymes, receptors, ion channels, transport proteins, structural proteins, nucleic acids, cell membranes). Drugs as analogs of natural compounds – neurotransmitters, hormones, substrates of enzymes. Quantitative methods for determining ligand binding and drug activity. Receptors as the main targets of drugs. G Protein-coupled receptors, intracellular signal transmission cascades: adenylyl cyclase and phospholipase C pathways. Receptor tyrosine kinases, MAPK/ERK kinase cascades. Ion channels, mechanisms of neuronal signal transmission. Intracellular receptors (nuclear receptors, transcryption factors). Lymphocyte T receptors and mechanisms of immunological responses. Enzymes as drug targets – application of inhibitors. Drug design: steps leading from the idea to introduction to the market: choosing the disease, choosing the target, development of biological assays. Finding a lead and structure optimization, pharmacophore, isosters. Combinatorial synthesis, computer-aided drug design, structure-activity relationship (SAR, QSAR, SBDD). Preclinical studies (toxicity) and clinical trials. Basic pharmacokinetics: absorption, distribution, metabolism and excretion (ADME) of drugs; doses and application of drugs. Anti-bacterial drugs (antibiotics) and anti-inflammatory drugs – history and mechanisms of action. Anti-cancer drugs, drugs acting on the blood system, drugs acting on the nervous system. Case study: Viagra, Lipitor, Prozac. Economic aspects of introducing drugs to the market, pharmaceutical companies, patents.
During seminars students solve problems related to the content presented during lectures. During last 2 classes students give presentations on selected topics from medicinal chemistry.
B. Laboratory:
Students perform 4 experiments:
1. Synthesis and purification of an analgesic drug (aspirin or paracetamol) and its spectroscopic characterization.
2. Identification of drug components by TLC.
3. Visualization o protein structure and protein-ligand interactions using PyMol.
4. Analysis of drug-target interactions by molecular docking using AutoDock 4.0.
Type of course
Course coordinators
Learning outcomes
A. Knowledge:
Student knows the groups of drug targets, the mechanisms of drug action and the origin of side effects.
Student knows the steps in drug development and its introduction to the market and methods used in this process.
Student understands the importance and principles of biological tests used for evaluation of drug candidates.
Student understands the connection between computational techniques and resources (literature and structural databases, molecular modeling), advanced synthetic procedures enabling preparation of desired compounds, biochemical and biological assays in drug development process.
Student understands the importance of patent protection of drug production processes.
B. Skills:
Student can design the synthesis of simple drugs from commercially available substrates and their purification.
Student can predict metabolic fate of selected drugs.
Student can analyze data from biological assays of drug candidate.
Student can carry out reactions of enzymatic degradation of selected drugs and selects methods to monitor them.
Assessment criteria
Requirements for passing the course
Lecture: final test (30 multiple choice questions), 50% of points required for passing.
Seminar: presentation (50% of grade) + points for solving problems, 50% of umber of point for presentation + 50% of the average of points for problems required for passing.
Laboratory: prelab tests (10 points each, 1/3 of grade) and lab reports (20 points each, 2/3 of grade), extra points for for technical skills and attitude during the class, 50% of points required to pass the course.
Bibliography
Basic textbooks:
1. G. L. Patrick, Chemia medyczna – podstawowe zagadnienia, WN-T, Warszawa, 2003.
2. G. L. Patrick, Chemia medyczna, PWN, Warszawa, 2019.
3. G. L. Patrick, Chemia leków, Krótkie wykłady, PWN, Warszawa, 2004.
4. J. Berg, J. L. Tymoczko, L. Stryer, G. J. Gatto, Biochemia, wyd. VIII, PWN, Warszawa, 2018.
Supplementary textbooks:
1. G. L. Patrick, An Introduction to Medicinal Chemistry, Oxford University Press, 6th edition, New York, 2017.
2. D. Steinhilber, M. Schubert-Zsilavecz, H. J. Roth, Chemia medyczna: cele leków, substancje czynne, biologia chemiczna, MedPharm Polska, Wrocław, 2012.
3. R. Silverman, Chemia organiczna w projektowaniu leków, WN-T, Warszawa, 2004.
4. Chemia leków, praca zbiorowa pod red. A. Zejca i M. Gorczycy, PZWL, Warszawa 2002.
Additional information
Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system: