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| Semester | fall semester 2026 |
| Course frequency | Irregular |
| Lecturers |
Alexander Flohr (alexander.flohr@unibas.ch)
Dennis Gillingham (dennis.gillingham@unibas.ch, Assessor) |
| Content | 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. |
| Learning objectives | 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. |
| Bibliography | 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. |
| Admission requirements | Knowledge in organic chemistry, introductory chemical biology, and undergraduate biochemistry. |
| Language of instruction | English |
| Use of digital media | No specific media used |
| Interval | Weekday | Time | Room |
|---|---|---|---|
| wöchentlich | Monday | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Date | Time | Room |
|---|---|---|
| Monday 14.09.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 21.09.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 28.09.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 05.10.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 12.10.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 19.10.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 26.10.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 02.11.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 09.11.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 16.11.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 23.11.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 30.11.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 07.12.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Monday 14.12.2026 | 09.15-12.00 | Chemie, Organische, Kleiner Hörsaal OC |
| Modules |
Module: Organic Chemistry (Master's Studies: Chemistry) |
| Assessment format | continuous assessment |
| Assessment details | Written exam (70%), group presentation (30%) |
| Assessment registration/deregistration | Reg.: course registration, dereg: cancel course registration |
| Repeat examination | no repeat examination |
| Scale | 1-6 0,5 |
| Repeated registration | as often as necessary |
| Responsible faculty | Faculty of Science, studiendekanat-philnat@unibas.ch |
| Offered by | Departement Chemie |