medicinal_chemistry_..
Transkrypt
medicinal_chemistry_..
ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ CHEMISTRY MEDICINAL CHEMISTRY II Level – MSc (3 semesters, 120 ECTS) PROGRAM 3 SEMESTERS Entry requirements: MSc Completed: Diploma of the I level studies in Chemistry, Biotechnology, Chemical Technology, Chemical Engineering Possible extension: Studies of the III level (PhD) Master Thesis, FinalExam Graduate: Medicinal chemistry is a scientific discipline at the intersection of chemistry and pharmacology. Medicinal chemistry involves the identification, synthesis and development of the compounds suitable for therapeutic use. Students are prepared to solve problems in the design of new drugs, analysis of existing drugs, their biological properties, and perfom the structure correlation analysis (QSAR). They are also trained in synthesis and structure analysis using the modern spectroscopic methods. Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ PLAN OF STUDIES 1st YEAR, SEMESTER 1 Obligatory courses: N o. Code 1 Subject/Module Theoretical and computational chemistry 2 Principles and practical aspects of medicinal chemistry 3 Principles of drug design 4 Advanced Organic Chemistry Contact hours/week L T 2 lab p s 2 2 1 1 5 Instrumental Analysis 1 6 Crystallography 2 7 Multistep organic synthesis 2 8 Physical Organic Chemistry 1 9 Foreign Language 10 Electives 3 1 4 2 CHS TSW ECTS Form of Assesment 60 150 5 ET 30 90 3 E 15 60 2 T 15 60 2 T 60 150 5 T 45 120 4 E 30 60 2 T 15 30 2 T 60 90 3 T 30 60 2 T CHS TSW ECTS Form of Assesment Optional courses // Choose one module No. Code Subject/Module TOTAL Contact hours/week L T lab p s 12 5 7 0 0 360 900 30 2 nd YEAR, SEMESTER 2 Obligatory courses: No. Code Subject/Module Contact hours/week L T lab p s CHS TSW Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ECTS Form of Assesment ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 1 Spectroscopic methods in medicinal chemistry 2 2 2 Molecular Modelling 1 2 3 Instrumental drug Analysis 1 2 4 Retrieval of technical and scientific information 1 60 150 5 ET 60 150 5 T 45 120 4 T 30 60 2 T 45 120 4 E 90 210 7 ET 60 120 4 T CHS TSW ECTS Form of Assesment 2 5 Medicinal Natural Products 1 2 6 Synthetic Organic Drugs 2 4 7 Research Laboratory 4 Optional courses // Choose one module No. Code Subject/Module TOTAL Contact hours/week L T lab p s 7 0 18 0 1 390 930 31 2 nd YEAR, SEMESTER 3 Obligatory courses: No. Code Subject/Module Contact hours/week L 1 Polymers in Medicine 2 2 Inorganic Drugs 2 3 Mathematical Methods in Drug Design 1 4 Graduate Laboratory 5 Graduate Seminar 6 Electives T lab p s 15 1 3 CHS TSW ECTS Form of Assesment 30 60 2 T 30 60 2 T 15 60 2 T 225 300 10 T 15 300 10 T 45 120 4 T Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Optional courses // Choose one module No. Code Subject/Module TOTAL MasterThesis: L T Contact hours/week L T lab p s 8 0 15 0 1 CHS TSW 360 900 ECTS Form of Assesment 30 TSW = 360 h 12 ECTS Final Exam: TSW= 240 h 8 ECTS La b p s L – Lecture T – Tutorials, l – laboratory, p – project, s – seminar, CHS TSW CHS – Contact Hours (organized), TSW – Total Student Workload (h), E – Exam, T – Test, CW – Course Work Optional courses // Choose one module No. 1 2 3 Code Subject/Module Combinatorial Chemistry Contact hours/week L T lab p s CHS TSW ECTS Form of Assesment 30 60 2 T 30 90 3 T 30 60 2 T 2 Terminoplogy in chemistry and biotechnology 2 Toxicology 1 Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Code RETRIEVAL OF SCIENTIFIC AND TECHNICAL INFORMATION Language: English Course: Basic Year (I), semester (1) Level: II Optional Prerequisites: Teaching:Traditional Lecturer: prof. W.A. Sokalski Lecture Tutorials Laboratory Project Seminar Hours / sem. (h) 30 Exam / Course work/T: CW ECTS 2 Workload (h) 60 Outcome: Critical analysis of scientific and technical information retrieved from literature and factographic data bases. Writing and editing scientific publications, cv’s, grant applications. Contents: Critical analysis techniques of information retrieved from literature (Current Contents, Science Citation Index, etc.) and factographic (CSD, PDB, Beilstein, etc.) databases. Writing and editing process of scientific publications, grant applications, CV’s. Ethical questions in science. Introduction, computer network services, Writing and editing scientific publications, ISI Current Contents and Science Citation Index databases, Structural CSD and PDB databases, genetic databases, patent databases, research grants, Job offers and fellowships, Ethical questions in science, CV’s, Beilstein database Literature: 1. D. Ridley, Finding Scientific Information, Information Retrieval:, Wiley, 2002. Code Advanced organic chemistry Language: English Year (I), semester (1) Level: II Prerequisites: Lecturer: Prof. Jacek Skarżewski Lecture Tutorials Hours / sem. (h) 15 Exam / Course work/T: T ECTS 2 Workload (h) 30 Course: Advanced Obligatory Teaching:Traditional Laboratory Project Seminar Outcome: Students should understand the reactivity of main groups of organic compounds. They should be able to apply the mastered mechanisms of organic reactions in order to explain the course of a moderately complex molecular transformation. Content: 1. Reaction intermediates, transition state, Hammond postulate Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 2. Reactions of carbonyl compounds: Alkylation of enolates and enamines 3. Aldol and Claisen condensations. Michael addition. 4. Reactions of organometallic compounds (Li, Mg, Zn,...). 5. Stereocontrolled reactions: diastereo- i enantiostereoselectivity 6. Reactions of organoboron, -silicon, and -tin compounds. 7. Reactions of organophosphorous compounds. 8. Reactions of organic sulfur and selenium compounds. 9. Stoichiometric and catalytic reactions of transition-metal compounds. 10. Radical and carbene reactions 11. Pericyclic reactions. 12. Selective methods for reductions of organic compounds. 13. Selective methods for oxidations of organic compounds. 14. Selective transformations and protections of functional groups. . Literature J. Clayden, N. Greeves, S. Warren, P. Wothers, Organic Chemistry, Oxford, 2000; J. McMurry, Chemia organiczna, tom 1 – 5, PWN, Warszawa, 2005; J.; Michael B. Smith, Jerry March, March’s Advanced Organic Chemistry, Wiley, 2000 L. G. Wade, Organic Chemistry, Prentice Hall, Upper Saddle River, NJ, 2006. Code Instrumental analysis Language: English Year (I), semester (1) Level: II Prerequisites: Lecturer: S. Bartkiewicz, Ph.D.,D.Sc. Lecture Tutorials Hours / sem. (h) 15 Exam / Course work/T: T ECTS 2 Workload (h) 30 Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Laboratory 45 T 3 90 Project Seminar Outcome: Fundamental knowledge of Instrumental Analysis. The course deals with the fundamental concepts and applications of instrumental techniques in chemical analysis. The Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ course covers some optic, spectroscopic, electroanalytical and chromatographic methods of analysis Content: 1. Introduction. Signal and noise statistical methods in analytical chemistry: errors, confidence limits and intervals analysis of variance, regression and correlation 2. Components of Optical Instruments 3. Optical methods 4. An Introduction to Ultraviolet/Visible Molecular Absorption 5. Spectrometry, Molecular Luminescence 6. Applications of Molecular Absorption 7. Electroanalytical Chemistry (Polarography, Potentiometry, Amperometry) 8. An Introduction to Chromatographic Separations, Gas Chromatography and Chromatography Liquid Literature 1.Cygański A., Metody spektroskopowe w chemii analitycznej, WNT 2002, Warszawa. 2. Cygański A., Metody elektroanalityczne, WNT 1995, Warszawa 3. Minczewski J., Marczenko Z., Chemia analityczna, tom 3, Analiza instrumentalna, PWN 1985, Warszawa 4. Szczepaniak W., Metody instrumentalne w analizie chemicznej, PWN 2004, Warszawa 5. Szmal Z., Lipiec T., Chemia analityczna z elementami analizy instrumentalnej , PZWL, 1997 Code crystallography Language: English Year (I), semester (1) Level: II Prerequisites: Course: Basic/Advanced Obligatory/Optional Teching:Traditional/Distance L. Lecturer: Prof. Veneta Videnova-Adrabińska, DSc Lecture Hours / sem. (h) 30 Exam / Course work/T: E Tutorials 15 T Laboratory Project Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego Seminar ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ ECTS Workload (h) 3 60 1 30 Outcome: Students will be provided with skills in crystal growing and with competence in crystal structure determination. The student should be acquainted with different diffraction techniques and familiar with structural data bases. They should be able to use this knowledge for solving of various analytical and structural problems in chemistry. Content: 1. Crystal lattices and lattice parameters: edges, directions, planes, unit cell, atom indexes 2. Crystal symmetry and crystal structure: symmetry elements, symmetry operations, point groups, space groups, crystal families and crystal systems; fourteen Bravais lattices. 3. Diffraction and crystal structure: geometry of X-Ray diffraction, interference by onedimensional lattice - the Laue equation, lattice planes and the Bragg equation, higher orders of diffraction, quadratic form of the Bragg equation; reciprocal lattice, the Ewald construction; the intensities of diffracted beams; structure factors – the atomic scattering factor, the structure factor; symmetry and reflection intensities; the temperature factor; symmetry of the diffraction patterns – the Laue groups; 4. Experimental techniques and X-ray diffraction methods for single crystal measurements: choice and mounting of a single crystal; the four circle diffractometer, area detector systems (CCDC cameras); measuring the diffraction patterns of single crystals; reflection profiles and scan type; structure solution methods (Pattersons methods, direct methods) the method of least squares for structure refinement, crystallographic R-values. 5. Other methods for structural research: powder X-Ray diffraction method: measuring the diffraction patterns on polycrystalline probes, determination of the lattice parameters and Bravais lattice type; electron microscopy and structure images; neutron scattering; electron scattering; protein crystallography. 6. Crystallization processes and methods for single crystal growth. 7. Depiction of crystal structures: metallic structures, ionic structures and structure building rules; cation-centered and anion-centered polyhedral representation of crystals, structures as nets; structural databases. Literature 1. Z. Bojarski, M. Gigla, K. Stróż, M. Surowiec, „Krystalografia”, PWN 2007. 2. Z. Trzaska Durski, H. Trzaska Durska, „Podstawy Krystalografii”, 2003. 3. Z. Kosturkiewicz, Metody krystalografii, Wydawnictwo Naukowe UAM, 2000. 4. W. Massa, Crystal Structure Determination, Springer, 2004. 5. R.J.D. Tilley, Crystals and Crystal Structures, Wiley, 2006. 6. G. Rhodes, Crystallography made crystal clear, Elsevier, 2006. Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Code Spectroscopic methods in medicinal chemistry Language: English Course: Basic/Advanced Year (I), semester (1) Level: II Obligatory/Optional Teaching:Traditional/Distance Prerequisites: Physics, Physical Chemistry L. Lecturers: R.Gancarz, prof, R.Latajka Dsc Lecture Tutorials Laboratory Project Seminar Hours / sem. (h) 30 2 Exam / Course work/T: E CW ECTS 3 2 Workload (h) 60 60 Outcome: Basic knowledge of spectroscopy and practical knowledge of essential spectroscopic techniques. Contents: Introduction to NMR spectroscopy – nucleus spin in magnetic field, chemical shift and spin-spin coupling, 1H NMR spectroscopy NMR spectroscopy – 1D spectra parameters – chemical shifts and factors which influence on it, coupling constants type H-X and X-Y and their influence on structure of molecules, 13C and 31P NMR spectroscopy. Application of NMR spectroscopy in structural and conformational studies of biomolecules – 2D spectra – COSY, TOCSY, HSQC, HMBC, NOESY, ROESY. Magnetic Resonance Imaging. Mass spectrometry – introduction, types of ionization and analyzers, connection with GC and LC, fragmentation. Mass spectrometry – comparison of macromolecules’ method of investigation – FAB, MALDI and ESI. IR spectroscopy – interpretation of spectra, basic absorption bands, application in structural studies – hydrogen bonding, Introduction to UV-Vis spectroscopy of organic compounds, monitoring of chemical reactions, electron spectroscopy in bioinorganic chemistry – application in coordination chemistry, CD spectroscopy – theoretical introduction, application in conformational studies of peptides and metal complexes, EPR spectroscopy – electron spin in magnetic field, parameters of spectra, application in studies of free radicals and metal complexes. Literature: 1. R.M. Silverstein, F.X. Webster „Spectrometric Identification of Organic Compounds“, J. Wiley&Sons 1996 2. H. Gunther “NMR Spectroscopy”, J. Wiley&Sons, 1994 3. J. M. Hollas, Modern Spectroscopy (Fourth Edition), Wiley & Sons, Ltd, 2004. 4. P.W. Atkins, Physical Chemistry, (Sixth Edition), Oxford University Press, Oxford Melbourne Tokyo 1998. Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Code theoretical and computational chemistry Language: English Year (I), semester (1) Level: II Prerequisites: Lecturer: Prof. Szczepan Roszak, Lecture Hours / sem. (h) 30 Exam / Course work/T: E ECTS 3 Workload (h) 60 Tutorials Laboratory Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Project Seminar Outcome: Basics of quantum chemistry are presented together with the emphasis of its practical application. The course provides knowledge of theoretical predictions of properties for molecules, complexes, and molecular materials, and also modeling of chemical processes. Content: 1. basic ideas and postulates of quantum mechanics 2. potential energy curves – molecular mechanics, chemical thermodynamics 3.simple model problems, potential barrier, hydrogen bond 4.harmonic oscillator – IR spectroscopy 5.rotator – microwave spectroscopy 6.hydrogen atom, spectroscopy of hydrogen atom 7. variational method 8.orbital approximation, Slater determinant 9. electronic structure of many-electron atoms, periodic table 10.Hartree-Fock method 11.Hartree-Fock-Roothan method 12.ab initio methods; atomic basis functions 13. chemical bond – electron population analysis Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 14. perturbation theory, intermolecular interactions 15. electron correlation, perspectives of theoretical chemistry Literature J. Sadlej, W. Kolos, Atom i Czasteczka, PWN; R. F. Nalewajski, Podstawy i Metody Chemii Kwantowej, PWN; L. Piela, Ideas of Quantum Chemistry, PWN; M. A. Ratner, G. C. Schatz, Introduction to Quantum Mechanics in Chemistry, Prentice Hall; Journal of Chemical Education, J. B. Foresman, A. Frisch, Exploring Chemistry with Electronic Structure Methods, Gaussian, Inc. Code physical organic chemistry Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: R.Gancarz, prof, J. Zoń, Ph.D.,D.Sc. Lecture Tutorials Hours / sem. (h) 15 Exam / Course work/T: T ECTS 2 Workload (h) 30 Laboratory Project Seminar Outcome: The course is supposed to give the basic knowledge of dynamics and energetics of organic transformations, rate comparisons between families of reactions, dynamic stereochemistry, conformational analysis, molecular recognition and catalysis. Content: 1. Stable and strain molecules. 2. Conformational analysis. 3. Electronic effects. Hammett plots. 4. Steric effects. Taft parameters. 5. Molecular mechanics. 6. Solutions and non-covalent binding force. 7. Molecular recognition. 8. Acid-base chemistry. Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 9. Stereochemistry. 10. Kinetics. 11. Primary and secondary kinetic isotope effects. 12. Reaction mechanism. 13. Catalysis. 14. Materials chemistry. Literature Aslyn E.V., Dougherty D.A., “Modern Physical Organic Chemistry”, University Science Books, Sausalito, California, 2006. Hammett L.P., „Fizyczna chemia organiczna”, PWN, W-wa, 1976. Schwetlick K., „Kinetyczne metody badania mechanizmów reakcji”, PWN, W-wa, 1975. Code Principles and practical aspects of medicinal chemistry Language: English Course: Basic/Advanced Year (I), semester (1) Level: II Obligatory/Optional Teaching:Traditional/Distance Prerequisites: L. Lecturer: Prof. Józef Oleksyszyn Lecture Tutorials Laboratory Project Seminar Hours / sem. (h) 30 Exam / Course work: E ECTS 3 Workload (h) 60 Outcome Description of the drug market and legal regulations. GMP. Generic drugs. Drug classification. New drug discovery methods. New experimental therapeutics. Gene therapy. siRNA. Monoclonal antibodies. New drugs on the market 2002-2006. Content: 1.Drug market, USA, EU, Poland. Generic drugs 2.Regulations concerning introduction of a new drug on the market 3.New drug discovery methods 4.Combinatorial chemistry 5.Drug classification 6.Enzyme inhibitors Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 7.Antagonist and agonist of the receptors 8.Drugs interacting with DNA 9.Drug metabolism 10.Prodrugs and drugs delivery systems 11-14. Examples of new drugs on the market 2002-2006 Literature: The organic chemistry of drug design and drug action – Richard B. Silverman; Academic Press, Inc., 1992 Comprehensive Medicinal Chemistry, Pergamon Press, 1994 Chemia Leków pod redakcją A. Zejca i M. Gorczycy, Wydawnictwo Lekarskie PZWL, Warszawa 1999 code medicinal natural products Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Prof. Jadwiga Sołoducho Lecturer: Prof. Jadwiga Sołoducho Lecture Hours / sem. (h) 15 Exam / Course work: E ECTS 2 Workload (h) 30 Tutorials Laboratory 30 T 2 60 Project Seminar Outcome: Students will become familiar with building blocks of herbal metabolic pathways and herbal secondary metabolism elements with a wide spectrum of properties (also therapeutic). Content: 1. Development in phytochemistry and natural products chemistry 2. Biological active compounds in herbs 3. Riches of sulphur compounds in natural products 4. Building blocks Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 5. Coumarins 6. Flavonoids and stilbenes 7. Terpenoids and steroids 8. Alkaloids 9. Glycosides 10. Anticancer natural products Literature: Medicinal natural products, Paul M. Dewick, John Wiley& Sons, LTD 2003; Organic chemistry, John Mc Murry, PWN, Warszawa 2000 Pharmacognosy, Stanisław Kohlmunzer, PZWL, Warszawa 2000 code principles of drug design Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: Prof. Paweł Kafarski Lecture Hours / sem. (h) 15 Exam / Course work: T ECTS 2 Workload (h) 30 Tutorials Laboratory Project Seminar Outcome: The techniques of drug design will be presented alongside with critical evaluation Content: 1. Economical aspects of implementation of research on new drug 2. Short history of drug design 3. Choice of target using AIDS as an example 4. Structural analogy as means of drug design 5. Design of alkylating and suicide enzyme inhibitors 6. Transition state analogues Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 7. Effectors of metalloenzymes 8. Drug targeting and applicators code instrumental drug analysis Language: English Year (I), semester (1) Level: II Prerequisites: Lecturers: Prof. Wiesław Żyrnicki, Marek Pohl, PhD Lecture Tutorials Laboratory Hours / sem. (h) 15 30 Exam / Course work: T T ECTS 2 2 Workload (h) 30 60 Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Project Seminar Outcome: Introduction to the monitoring and analysis of pharmaceutical products. Knowledge of chemical, physical and biochemical methods used in drug analysis, with a special attention to spectroscopic and chromatographic techniques. Identification and quantification of organic and inorganic species. Development of analytical skills in the area of main and trace components of pharmaceuticals. Quality control and quality assurance. Content: 1. Introduction to drug analysis 2. Analytical process, procedures and techniques. Analytical figures of merit. Validation 3. Introduction to spectroscopic methods in pharmacy 4. Atomic and molecular spectroscopy methods 5. Methods of structure analysis of drug components (IR, Raman, NMR, XRD) 6. Electrophoresis and chromatography 7. Sample preparation methods. Trends in development of drug analysis 8. Summary. Written test Literature: 1. Watson D.G., Pharmaceutical Analysis. Churchill Livingston, Edinburgh, 2005 2. Pharmacopeias (US, European, WHO) 3. Kellner R. (Ed.), Analytical Chemistry. John Wiley & Sons, London, 2004 4. Skoog D.A., West D.M., Holler F.J., Fundamentals of Analytical Chemistry. Saunders College Publishing, 2003 Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ code synthetic organic drugs Language: English Year (I), semester (1) Level: II Prerequisites Lecturers: : Prof. Roman Gancarz, Izabela Pawlaczyk, PhD Lecture Tutorials Laboratory Hours / sem. (h) 30 60 Exam / Course work: E T ECTS 3 4 Workload (h) 60 120 Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Project Seminar Outcome: Knowledge of fundamental classes of drugs, their mode of action and their analysis Content: 1. Reaction mechanisms in organic chemistry and drug action 2. Chirality and biological activity of drug. 3. Drug target binding forces, role of molecular recognition in drug design and drug action. 4. Kinetics and thermodynamics in drug action 5. Proteins as drug targets – enzymes and receptors, peptidomimetics. 6. Drugs acting on carbohydrates and lipids and their metabolism. 7. Drugs acting on DNA and RNA and their metabolism, oligonucleotide therapeutics 8. Cardiovascular agents 9. Drugs affecting hormonal system. 10. Drugs affecting immune system 11. Drugs affecting nervous system. 12. Chemotherapeutic drugs 13 Bio NMR, MS in drug discovery 14 Absorption, distribution, administration and toxicity of drugs, drug metabolism, prodrugs 15. New drugs. Literature: Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ The organic chemistry of drug design and drug action – Richard B. Silverman; Academic Press, Inc., 1992 Comprehensive Medicinal Chemistry, Pergamon Press, 1994 Chemia Leków pod redakcją A. Zejca i M. Gorczycy, Wydawnictwo Lekarskie PZWL, Warszawa 1999 code molecular modeling Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance Prerequisites: L. Lecturers: Prof. Andrzej Sokalski, Paweł Kedzierski, PhD, Edyta Dyguda-Kazimierowicz, PhD Lecture Tutorials Laboratory Project Seminar Hours / sem. (h) 15 30 Exam / Course work: T T ECTS 2 2 1 Workload (h) 30 60 30 Outcome: Basic understanding of computational approaches used to describe and explain the chemical structure, its properties and structure-function relationships. Content: 1. Introduction, molecular graphics 2. Molecular model building and visualization 3. Structural databases and their use in molecular modeling 4. Overview of computational techniques of quantum chemistry 5. Elements of the theory of intermolecular interactions 6. Force fields and molecular mechanics 7. Predicting molecular structure, conformational analysis 8. Predicting physical and chemical properties of molecules 9. Modeling of molecular aggregates 10. Modeling chemical reactions 11.Molecular dynamics Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 12.Drug design techniques 13. Catalyst design techniques 14. Homology modeling 15.Written exam Literature: 1 Basic literature: A.R.Leach, Molecular Modelling: Principles and Applications (2nd Edition), Prentice Hall; ISBN: 0582382106, 2001. 2: T. Schlick, Molecular Modeling and Simulation, Springer, 2002 3 L. Piela, Ideas of Quantum Chemistry, Elsevier, 2006 code research laboratory Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: supervisor Lecture Hours / sem. (h) 60 Exam / Course work: T ECTS 4 Workload (h) 120 Tutorials Laboratory 4 Project Seminar 4th SEMESTER Code POLYMERS IN MEDICINE Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: Prof. Marek Bryjak Lecture Hours / sem. (h) 30 Exam / Course work/T: T Tutorials Laboratory Project Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego Seminar ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ ECTS Workload (h) 2 60 Outcome: Advantages and opportunities to use polymers in biotechnology and medicine. General overview of polymers, their synthesis, structure and properties, use of polymers in selected areas? of medical treatment. Contents: History of polymers, impact of polymers to our life, Polymerisation, copolymerisation, grafting, plasma polymersation, .Molecular weights, number and weight averaging, polydispersity, methods of molecular weight evaluation, Solution of polymers. Flory-Huggins model, Blends of polymers, block copolymers, interpolymers. Phase transitons, amorphic and semicrystaline polymers .Surface properties of polymers, surface energetics, methods of surface investigations. Diffusion in polymers, polymer membranes. Artificial organs (kidney, liver, lung, pancrease). Polymer orthopedic elements, polymers in dentistry.Tissue engineering, scaffolds, Controlled release drugs, targeted drugs. Polymers with improved affinity, molecularly imprinted materials. Surgeon materials, smart polymers, polymers with memory. Polymeric supports and carries for bioactive molecules. Literature: 1.H.G.Elias, Macromolcules, Plenum Press, New York 1984, 2.L.Sperling, Polymer physicochemistry, Elsevier, New York, 1992 code inorganic drugs Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: prof. Danuta Michalska-Fąk Lecture Hours / sem. (h) 30 Exam / Course work: T ECTS 2 Workload (h) 60 Tutorials Laboratory Project Seminar Outcome: The aim of this course is to review the diagnostic and therapeutic applications of inorganic compounds (metal complexes and radioisotopes) in medicine. It develops an understanding of the basic mechanisms of the modern diagnostic techniques: Magnetic Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Resonance Imaging (MRI), Positron Emission Tomography (PET), nuclear medicine (SPECT) and the role played by metallopharmaceuticals in these techniques. Content: 1. Classification of drugs, Drug discovery, design and development 2. Clinical trials. Development of inorganic drugs. 3. Diagnostic methods: X-ray and application of inorganic contrasts agents. Magnetic Resonance Imaging (MRI) technique 4. The use of Gadolinium(III) complexes as the T1-type contrast agents and new T2-contrast agents in MRI and MR angiography techniques. 5. Positron Emission Tomography (PET) and the use of radiotracers: Fluorine-18, Copper-64, Rubidium-82 and Gallium-68 isotopic compounds as positron emitters. 6. Nuclear medicine (SPECT) and the use of radionuclides (gamma emission): Technetium-99m, Gallium-67 and Indium-111 compounds. 7. Therapeutic radiopharmaceuticals (Samarium-153 complex) and Boron- Neutron Capture Therapy (BNCT). 8. The origin of cancer and various types of chemotherapy 9. Cisplatin and its mechanism of action in anticancer therapy 10. New generations of platinum drugs. Search for an orally active drug 11. Non-platinum compounds in anticancer therapy. Ruthenium complexes in therapy of cancer metastases. 12. Bismuth compounds in medicine. Activity against Helicobacter pylori 13. Vanadium salts and coordination compounds as insulin mimics for diabetes treatment 14. Chrysotherapy - gold complexes in treatment of rheumatoid arthritis 15. Perspectives of Medicinal Inorganic Chemistry Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Literature: 1.L. Sessler, S. R. Doctrow, T. J. McMurry, S.J. Lippard, Medicinal Inorganic Chemistry, Oxford University Press, 2005. 2) Concepts and Models in Bioinorganic Chemistry, Ed. H Kraatz, N. Metzler-Nolte, 2006. (review article) by Thompson and Orvig: „Medicinal Inorganic Chemistry”, pages 25 - 46. 3 G.L. Patrick, Chemia medyczna. Podstawowe zagadnienia. II wyd. WNT Warszawa, 2003 4) Metallopharmaceuticals I, DNA Interactions, M.J. Clarke, P.J. Sadler , 1999. 5) Metallopharmaceuticals II, Diagnosis and Therapy , M.J. Clarke, P.J. Sadler 1999. code mathematical models in drug design Language: English Year (I), semester (1) Level: II Prerequisites: Lecturer: Prof. Roman Gancarz Lecture Hours / sem. (h) 15 Exam / Course work: T ECTS 2 Workload (h) 30 Tutorials Laboratory Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Project Seminar Outcome: The goal of the course is to get the knowledge of applying the rational way of drug design using simple correlation analysis, as well as advanced pattern recognition methods. Content: 1.Introduction to modelling in science and especially in chemistry 2. Satatistics in data analysis 3. Structural descriptors of molecules 4. Correlation analysis in drug design. Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ 5. Regression medels, Hansh, Kubynyi, Free Wilson approaches 6. Principal component analysis, linear and nonlinear mapping 7. Classification and classifiers, clustering methods, 8. Pattern recognition methods 9. Neural network application in structure property analysis. Literature: code graduate laboratory Language: English Year (I), semester (1) Level: II Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: supervisor Lecture Tutorials Hours / sem. (h) Exam / Course work: ECTS Workload (h) Laboratory 60 T 10 120 code graduate seminar Language: English Year (I), semester (1) Level: II Tutorials Seminar Course: Basic/Advanced Obligatory/Optional Teaching:Traditional/Distance L. Prerequisites: Lecturer: Prof. Roman Gancarz Lecture Hours / sem. (h) Exam / Course work: ECTS Workload (h) Project Laboratory Project Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego Seminar 15 T 10 30 ROZWÓJ POTENCJAŁU I OFERTY DYDAKTYCZNEJ POLITECHNIKI WROCŁAWSKIEJ Projekt współfinansowany ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego