Problem 2
Resistance to your new potent antibacterial drug (1) was shown to be the result of a single-point genetic mutation in the target enzyme such that an important active site lysine residue was mutated to an aspartate residue. Suggest a simple way to proceed toward the design of a new antibacterial drug against the resistant strain.
Problem 3
Augmentin is a medicine that combines amoxicillin, a \(\beta\)-lactam antibiotic, with clavulanate, a \(\beta\)-lactamase inhibitor. Why is it important that the two compounds have similar pharmacokinetics (e.g., oral bioavailability and plasma half-life) in humans?
Problem 4
When might it be a disadvantage to inhibit a drugdestroying enzyme?
Problem 6
If drug resistance to an antibacterial compound arises from expression of a new enzyme in the resistant organism that destroys the drug, what three approaches could you take to combat the resistance?
Problem 7
One mechanism of drug resistance is that the organism has a genetically altered enzyme. How does this lead to drug resistance?
