1 Predict, giving a reason for the prediction, the most likely general effect of the stated structural change on either the in situ stability or the pharmacological action of the stated drug.
(a) The introduction of ortho ethyl groups in dimethylaminoethyl 4-aminobenzoate.
(b) The replacement of the amino group in the CNS stimulant amphetamine (PhCH2CH(NH2)CH3) by a trimethylammonium chloride group.
(c) The replacement of the ester group in the local anaesthetic ethyl 4-aminobenzoate (benzocaine).
2 State the general factors that need to be considered when designing a drug.
3 Explain the meaning of the terms: (a) lead compound, (b) dosage form, (c) enteral administration of drugs, (d) drug regimen, (e) prodrug, (f) pharmacophore and (g) excipient.
4 Define the meaning of the terms pharmacokinetic phase and pharmacodynamic phase in the context of drug action. List the main general factors that affect these phases.
5 The drug amphetamine (PhCH2CH(NH2)CH3) binds to the protein albumin in the blood stream. Predict how a reduction in pH would be expected to influence this binding? Albumin is negatively charged at pH 7.4 and electrically neutral at pH 5.0.
6 Discuss the general effects that stereoisomers could have on the activity of a drug. Draw the R and S isomers of the anaesthetic ketamine. Indicate which of the structures you have drawn is mainly responsible for its anaesthetic activity.
7 Suggest strategies for improving the stability of compound A in the gastrointestinal tract. What could be the general effect of these strategies on the pharmaceutical action of compound A?
8 Explain the meaning of the term receptor.
9 What are the Lipinski rules? Use the Lipinski rules to determine which of the following compounds are likely to be orally bioavailable. Give a reason for your decision. (Note: the log P values are imaginary but should be taken as real for this question only!)
10 List the desirable requirements for a lead.
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