上海交通大学：《药物化学》课程教学资源（课后题库）Chapter 6 Cental Nervous System Drugs

1.Despite barbiturates,hydantoins and succinimides,the antiepiliptics possess common structure.Please identify the possible common structure of different types of antiepileptics. 2.Diazepam and Carbamazepine could be converted into their "me-better"drugs Oxazepam and Oxcarbazepine by attachment of hydroxyl groups respectively.Can you specify the mechanism of this group to maintain the advantage of shorter duration for Oxazepam and lower toxicity for Carbamazepine? 3.How to understand the rationally designed MTDLs(multi-target-directed ligands)against Alzheimer's disease are conceptually very different from unselective drugs of the past or from the so-called 'dirty drugs'? 4.Could DA receptor agonist apomorphine be described as conformational constrained analogue of dopamine?Figure out the structural motif of dopamine from that of apomorphine. 5.Compare the structures of MAO-B,COMT and amino acid decarboxylase inhibitors with that of dopamine or L-dopa,can you specify how these inhibitors with additional critical functional groups could maintain their preferable activities over their natural substrates?

1. Despite barbiturates, hydantoins and succinimides, the antiepiliptics possess common structure. Please identify the possible common structure of different types of antiepileptics. 2. Diazepam and Carbamazepine could be converted into their "me-better" drugs Oxazepam and Oxcarbazepine by attachment of hydroxyl groups respectively. Can you specify the mechanism of this group to maintain the advantage of shorter duration for Oxazepam and lower toxicity for Carbamazepine? 3. How to understand the rationally designed MTDLs (multi-target-directed ligands) against Alzheimer's disease are conceptually very different from unselective drugs of the past or from the so-called 'dirty drugs'? 4. Could DA receptor agonist apomorphine be described as conformational constrained analogue of dopamine? Figure out the structural motif of dopamine from that of apomorphine. 5. Compare the structures of MAO-B, COMT and amino acid decarboxylase inhibitors with that of dopamine or L-dopa, can you specify how these inhibitors with additional critical functional groups could maintain their preferable activities over their natural substrates?