MedChem exam content


            Explain terms pharmacodynamics, pharmacokinetics, bioavailability

            Uptake routes for drugs

            Body fluid compartments, volume of distribution

            Drug absorption in the intestinal tract, transport through epithelial cells

            Blood-brain barrier

            Efflux pumps

            Binding to plasma proteins

            Metabolic phase 1 and 2

            Elimination of drugs


            Drug toxicity

            Phases of drug development

            Target identification

            Biophysics of drug-receptor interactions

            Polar surface area

            Binding affinities

            Properties of fragments,leads and drugs

            Lipinski rules

            Screening techniques

            Virtual screening


            QSAR relationsships

            Hansch equation (which terms are included?)

            3D QSAR


            changing solubility


            drug delivery systems

            fragments-based drug design, SAR-by-NMR

            properties of fragments vs drugs

            rational drug design

            methods (roughly): X-ray,NMR,SPR, Ultracentrifugation, ITC, DSC, Thermafluor

            most important receptors, mode of action, structures (roughly)

            dose-response curves, binding curves, definition of Kd, agonist, antagonist (full and partial, inverse ag.)

            determination of Kd

            antibacterials: strategies, membranes of mammalian, gram +/- cells, action and targets of antibiotics

            antiviral drugs:strategies, HIV/influenza treatments

            anticancer drugs: hallmarks of cancer, mode of action of anti-cancer drugs, antibodies

            anti-inflammatory drugs: immune response, innate and adaptive immune system, pain mediators

MedChem exam content (part D. Obrecht)

1.      Introduction: The Drug Discovery and Development Process

        Drug absorption, distribution and elimination



2.      Lead Discovery and Lead Optimization-Drugability

        Drugability: Lipinskis rule of 5

        Drugability parameters

        Shape analysis

        Is there a difference between leads and drugs? the rule of 4

        Fragments: the rule of 3

        Privileged structural elements


        Unwanted molecular properties

3.      Combinatorial and Parallel Synthesis in Medicinal Chemistry

        Historical background-objective

        The role of combinatorial chemistry and parallel synthesis in drug discovery

        Compound mixtures versus single compounds

        Solid phase synthesis versus synthesis in solution

        Parallel versus split-mixed synthesis

4.      Combinatorial synthesis of Biopolymers

        Linear, modular synthesis of biopolymers

        Solid-phase synthesis of polypeptides; peptoids; oligosaccharides

        Parallel synthesis vs combinatorial synthesis: split-mixed synthesis

        Examples for solid-phase synthesis: Split-mixed synthesis; tagging strategies; pin synthesis; tea-bags; photolithography; radiofrequency tags; binary encoding; factor Xa inhibitors; thrombin inhibitors; inhibitors of protein-protein interactions; hot spots and o-rings; synthesis of a-helix mimetics; phage libraries;

        Peptide mimetics

5.      Strategies for the Synthesis of Small Molecule Libraries

        Library synthesis planning

        Synthesis strategies

        Classical multi-component reactions (MCRs)

        Sequential multi-component reactions (SMCRs)

        Diversity-oriented synthesis (DOS)

        Collective synthesis of natural products

        Fragment-based lead discovery

        Dynamic Combinatorial Synthesis;

        Target-guided synthesis (TGS)

        Disulfide thethering; click chemistry

        Most important reactions used in parallel and combinatorial synthesis

        Most important building blocks used in parallel and combinatorial synthesis

        Parallel and/or combinatorial synthesis

           Parallel work-up