Pharmaceutical Chemistry/ Medicinal Chemistry Pharmaceutical ...

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Hartke/Hartke/Mutschler/Rücker/Wichtl: Arzneibuch-Kommentar (Deutsches und. Europäisches Arzneibuch). - Mutschler, Arzneimittelwirkungen.

Pharmaceutical Chemistry/ Medicinal Chemistry Pharmaceutical Chemistry (Joint Lecture) (Pharmazeutische Chemie)

Lecture: 4 hours per week (winter and summer semester) ECTS credits: 15 Topics : - Chemotherapy of infections: antibacterial, antifungal and antiviral agents. - Anticoagulant and thrombolytic drugs. - Hormones: Adenohypophyseal hormones, hypothalamic releasing factors; thyroid drugs; estrogens and gestagens; oral contraceptives; pregnancy tests; androgens; insulins, oral hypoglycenic agents; pharathyroid hormone - vitamin D. - Vitamins: B-vitamins, ascorbic acid; vitamins A, E. - General anesthetics; local anesthetics; hypnotics; antiepileptics; Parkinson´s disease; opioid analgetics; NSAID´s; antitussive agents; antiemetic agents. - Radiopharmaceuticals Literature : Goodman-Gilman, The Pharmacological Basis of Therapeutics; Roth et al., Pharmaceutical Chemistry (both also available in English) Topics : Receptors (structures, signalling pathways, hormones, neurotransmitter, ligand receptor interactions); drugs acting on the CNS (neuroleptics, antidepressants, anxiolytics, hypnotics, antiepiletics), drugs affecting cholinergic mechanisms (cholinergics, anticholinergics, AChE inhibitors etc.), drugs affecting adrenergic mechanisms (direct and indirect sympathomimetics, antagonists), antihypertensives and drugs used for the treatment of myocardial ischemia (alpha- and beta-adrenoceptor antagonists, other sympatholytic agents, calcium channel antagonists, potassium channels activators, ACE inhibitors, angiotensin II antagonists, renin inhibitors, organic nitrates, other vasodilators), antiarrhythmics, positive inotropic drugs, diuretics, drugs used in the treatment of hyperlipoproteinemias, histamine receptor agonists and antagonists, 5-hydroxytrypamine receptor agonists and antagonists, antiulcer drugs, laxatives, antiasthmatics, anticancer drugs, drugs used for immunomodulation. Literature : - Auterhoff/Knabe/Höltje, Lehrbuch der Pharmazeutischen Chemie - Roth/Fenner, Pharmazeutische Chemie III - Krogsgaard-Larsen/Bundgaard, A Textbook of Drug Design and Development - Hartke/Hartke/Mutschler/Rücker/Wichtl: Arzneibuch-Kommentar (Deutsches und Europäisches Arzneibuch) - Mutschler, Arzneimittelwirkungen - Löffler/Petrides, Biochemie und Pathobiochemie no assessment

Special regulations for exchange students : Complementary seminars for foreigners in English Arrangements for earning course credit for partial fulfillment can be made with lecturers.

Computer-Aided Methods in Drug Research (Computergestützte Methoden in der Arzneimittelforschung) Lecture: 3 hours per week (winter semester) ECTS credits: 3 Topics : General strategies of computer-aided rationalization in drug design. Quantitative structure-activity relationships (QSAR): Probability models of linear freeenergy relationships in biological and model systems; hydrophobic, electronic, and steric effects and their description in molecules; demonstration at the PC of methods(Hansch analysis, fragment regression, principal component analysis) and drug design examples (hypnotics, ligand-protease binding, structure-hydrophobicity relationships, series design). Molecular modeling: idealized and real models of ligand-receptor interactions, modeling strategies in drug design (receptor mapping, docking); molecules "in computro", force field methods; computer demonstrations with SYBYL (Tripos Ass.) at a SG Indigo2 workstation (conformational analysis, electrostatic potentials, search for active conformations, template forcing, pharmacophore search, docking, volume comparisons, 3D QSAR approaches). Literature : - Scheler, Allgemeine Pharmakologie - Böhm/Klebe/Kubinyi, Wirkstoffdesign - Kubinyi, QSAR: Hansch Analysis and Related Approaches - Höltje/Folkers, Molecular Modeling - Franke, Theoretical Drug Design Methods - Silverman, Medizinische Chemie no assessment

Molecular Modeling (Molecular Modeling)

Practical Course: 6 hours per week (summer semester) ECTS credits: 6 Topics : Introductional lectures: molecular modeling in chemistry, biochemistry and drug design, idealized and real models of ligand-biomolecule interactions; modeling strategies and software components; molecules "in computro"; molecular mechanics, Tripos force field, energy minimization algorithms.

Computer exercises with SYBYL (Tripos Ass.) at 10 SG Indy workstations (1-2 students at each Indy): small molecule sketching; energy calculation and minimization; working with molecular spreadsheets and databases; conformational analysis, distance maps; electrostatic potentials; pharmacophore search by active analog approaches, volume comparisons; Monte Carlo and molecular dynamics simulations, simulated annealing; biopolymer modeling (peptide sketching, secundary structure analysis, ligand-protein docking); semiempirical quantum-chemical methods (MOPAC): analysis of molecular orbitals; calculation of structure-property relationships (e.g., charges, aromaticity, reactivity and reaction mechanism). Literature : - Böhm/Klebe/Kubinyi, Wirkstoffdesign - Höltje/Folkers, Molecular Modeling - Burkert/Allinger, Molecular Mechanics - Leach, Molecular Modelling - Principles and Applications - Cohen, Guidebook on Molecular Modeling in Drug Design - Eliel/Wielen, Stereochemistry of Organic Compounds Method of assessment : practical examination

Pharmaceutical Chemistry II (Methods of the Pharmacopoeia) (Pharmazeutische Chemie II (Arzneibuchuntersuchungen)) Practical Course: 16 hours per week (winter semester) ECTS credits: 14 Topics : Characteristic data of fats and oils Drug monographies: menadione, acetylcysteine, metronidazole, pyridoxine, benzocaine, phenobarbital, phenylbutazone, theophyllin, tetracaine, paracetamole, sulfaguanidine, allopurinol, chloroquine, niclosamide Literature : Europäisches Arzneibuch 1997 Kommentar zum Deutschen Arzneibuch 10 European Pharmacopoeia Method of assessment : written examination

Pharmaceutical Chemistry III (Toxicology, Drug Analysis) (Pharmazeutische Chemie III (Toxikologie, Arzneimitteluntersuchung))

Practical Course: 20 hours per week (summer semester) ECTS credits: 16 Topics : The focal point of this course is the qualitative analysis of mixtures of pharmacologically active compounds (approximately 250 molecules) and 23 supporting materials (carriers) . The course is divided into four sections: a) identification of unknown (unmixed) substances, b) analyses of combinations of up to 3 active compounds plus two carriers , and c) analyses of combinations of up to 5 compounds plus 3 carriers. In sections a) and b), the carriers are varied. Thus, the students become familiar with the analyses of solid, semi-solid, and liquid pharmaceuticas. In section c) only solid materials are analysed. In addition to chemical separation procedures (Stas-Otto separation, e.g.), mainly TLC and IR-spectroscopy are used. - In toxicological analyses students have to isolate and identify toxicologically relevant compounds in food. - Analyses are evaluated by a point system. The practical part of the course has been finished successfully if 75% of the maximal sum of points have been accomplished. - During the course there are three examinations: 1) a written test at the beginning showing that the students have proper knowledge in organic chemistry and in safety regulations necessary for the course; 2) an oral examination following section b) , and 3) a written test at the end of the course comprising chemistry and pharmacology of the drugs and of the chemistry of the carriers, being part of the course, as well as of the contents of the corresponding lectures in pharmaceutical / medicinal chemistry, and the knowledge offered in weekly seminars. Seminars: a) given by the students; b) given by invited professors / lectures being experts in special areas; c) concerning medicinal data banks. Literature : Klaus Müller, Toxikologie und Arzneimitteluntersuchungen, Einführung in das Praktikum Pharmazeut. Chemie III (Regensburg University). Method of assessment : written examination