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79188-01 - Lecture: Medicinal Chemistry (3 CP)

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

Dates

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

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