Order unknown for the following questions:

- Frage 1a: Why is michaelis menten constant important for substrates binding to enzymes. Explain what information you can get from it.
- Frage 1b: Explain the importance of a low Koff of a drug
- Frage 1c: Calculate Koff if given Kon and Ki.
- Explain Prodrug in 2-3 sentences (2p). Mark the prodrug in the structure. (1p)
- Why is the activity of Glucuron Transferase a problem for medicinal chemists? (1p)
- What problems does drug discovery have with b-lactam drugs?
- …..? circle where cleaved by …? (isch es en pro drug gsi oder um de metabolismus gange? Penicillin G mit grosser gruppe an 5 ring nach CO2R)
- Draw the metabolites of different drugs
- Definition non-classical bioisostere and what is the non-classical bioisostere of -COOH compared to -Ph, -C(CH3)3, -Br and -five ring with multiple N
- MW > 460, logP=4, 3 HBD, 6 HBA : how is the bioavailability - explain
- drug targeting Adenosine deaminase given. infer possible target.
- draw nat. ligand drawing
- Defintion of Auxophore
-Why can PK properties of drugs be changed using auxophore?
- Explain induced fit theory
- What is drug drug interaction?
- 2 Medikamente ( Antivral/Enzyme inhibitor) gegeben. werden von Cyp3A4 verstoffwechselt. Wieso problem, wenn patient gleichzeitig phenobarbital (inducer) erhält. Was ist die Konsequenz, bei gleichzeitiger Einnahme von Cyclosporin (Hemmer) (no worries in liste gegeben.)
- Antiviral given. How will this drug look like after metabolisation? (It was a NRTI, so you had to add the phosphate groups)
- Drug given (antiviral?) what interaction with Asp(?) in enzyme? (X-ray picture given)
- Glycin (?) group was added and gave better potency, why?
- Why Guanidyl (?) group not favourable for optimissation process?
- Cefalothin beta-lactam drug: draw 2 metabolites
- Why are infectious disease easy to target? 2 reasons needed for the points
- 4 main activities in drug discovery?
- why are metabolites dangerous (Why are metabolites challenging for the development of new drugs)?
- typical steps to identify metabolites
- Explain SAR
- why are natural ligands good lead structure? how can we approaches to discover lead structure?
- Struktur eines natürlichen liganden gegeben. 1 positive argument, etwas negatives bei verwendung von natürlichen liganden als lead?
- What steps does the metabolism has?
- Drug has following properties (460 D, 3 HBD, 6 HBA, logP 4.0). What can you say about the oral bioavailability of the drug?