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79188-01 - Vorlesung: Medicinal Chemistry (3 KP)
| Semester | Herbstsemester 2026 |
| Angebotsmuster | unregelmässig |
| Dozierende |
Alexander Flohr (alexander.flohr@unibas.ch)
Dennis Gillingham (dennis.gillingham@unibas.ch, BeurteilerIn) |
| Inhalt | This course provides a comprehensive introduction to modern medicinal chemistry, covering the principles and strategies used to discover, design, and optimize small-molecule drugs. Starting from the molecular basis of drug–target interactions, we will follow the path from initial hit compounds through lead optimization to clinical candidates. You will learn to think like a medicinal chemist: balancing potency, selectivity, and drug-like properties in a multi-parameter optimization framework. The course emphasizes modern developments including covalent drug design, targeted protein degradation, and computational approaches, and concludes with integrative case studies that connect all concepts to real drug discovery programs. |
| Lernziele | By the end of this course, you will be able to: 1. Explain the stages of the drug discovery pipeline and the role of medicinal chemistry at each stage. 2. Analyze drug–target interactions at the molecular level, including thermodynamic and kinetic contributions to binding. 3. Design and interpret structure–activity relationship (SAR) studies for hit-to-lead and lead optimization campaigns. 4. Predict and address ADME liabilities using common medicinal chemistry strategies such as bioisosteric replacement, metabolic blocking, and prodrug design. 5. Evaluate modern drug design approaches including covalent inhibitors, PROTACs, molecular glues, and RNA-targeting small molecules. 6. Learn about various computational and data-driven tools (molecular docking, FEP, AI/ML) to support drug design decisions. 7. Critically analyze a complete drug discovery case study, articulating the rationale behind key medicinal chemistry decisions. |
| Literatur | The Practice of Medicinal Chemistry: C. G. Wermuth et al., 5th Edition Comprehensive reference; excellent for in-depth reading on specific topics. An Introduction to Medicinal Chemistry: G. L. Patrick, 7th Edition Accessible and well-illustrated; a good companion throughout the course. The Organic Chemistry of Drug Design and Drug Action: R. B. Silverman & M. W. Holladay, 3rd Edition Strong on mechanisms; particularly useful for Blocks 1–3. Additional primary literature and review articles will be provided for each weekly topic on the course platform. |
| Teilnahmevoraussetzungen | Knowledge in organic chemistry, introductory chemical biology, and undergraduate biochemistry. |
| Unterrichtssprache | Englisch |
| Einsatz digitaler Medien | kein spezifischer Einsatz |
| Intervall | Wochentag | Zeit | Raum |
|---|---|---|---|
| wöchentlich | Montag | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
Einzeltermine
| Module |
Modul: Organic Chemistry (Masterstudium: Chemie) |
| Prüfung | Lehrveranst.-begleitend |
| Hinweise zur Prüfung | Written exam (70%), group presentation (30%) |
| An-/Abmeldung zur Prüfung | Anm.: Belegen Lehrveranstaltung; Abm.: stornieren |
| Wiederholungsprüfung | keine Wiederholungsprüfung |
| Skala | 1-6 0,5 |
| Belegen bei Nichtbestehen | beliebig wiederholbar |
| Zuständige Fakultät | Philosophisch-Naturwissenschaftliche Fakultät, studiendekanat-philnat@unibas.ch |
| Anbietende Organisationseinheit | Departement Chemie |