MEDICINAL CHEMISTRY 1

UNIT 1
10 MARKS
1. a) Explain how the following physicochemical properties affect drug action.
i) Hydrogen bonding ii) Geometrical isomerism iii) Protein binding b)
Define the process of metabolism? Illustrate the factors affecting metabolism
of drugs.
2. Explain in detail about Phase II metabolism reactions with examples.
3. Explain the following physiochemical properties related to the biological
action. a) Hydrogen bonding b) Optical and geometrical isomerism.
4. a) List out the physicochemical properties that influence biological action.
With suitable examples explain how the following properties affect drug
absorption. (6) i) Solubility ii) Ionization iii) Hydrogen bonding. b)Write
briefly on enzyme system involved in I Phase metabolism of drugs. (4)
5. Explain the various types of Phase I biotransformation pathways.
6. Discuss the following metabolic reactions with examples (a) Acetylation (b)
Glucuronidation (c) Sulfation.
7. Enumerate the various physicochemical properties that influence the
biological activity and explain any two of them in detail.
8. A) Explain how the following properties influence the biological action a)
Partition coefficient. B) hydrogen bonding. B) Explain Phase I drug
metabolism with examples.

5 MARKS
1. Explain the factors affecting drug metabolism including stereochemical
aspects
2. Explain Phase I metabolism of hepatic cytochrome P 450 system
3. Explain protein binding with examples.
4. Outline the various factors that influence metabolism.
5. Explain chelation and bioisoterism* with examples.
6. Discuss in detail the various stereochemical aspects of drug metabolism.
7. Write a note on chelation and solubility
8. Describe the Phase I Metabolism.
UNIT 2
10 MARKS
1. a) What are drug receptors? Write a note on the different types of receptors
available for drug action. b) Define and classify adrenergic antagonists with
suitable examples. Write the synthesis and uses of i) Tolazoline ii)
Propranolol.
2. Discuss the structural activity relationship of β phenyl ethyl amines of direct
acting sympathomimetics.
3. a) What are adrenergic neurotransmitters? Classify them with suitable
examples.(3) b) Write in detail about biosynthesis and catabolism of
catecholamines. (3) c) Mention the use and synthesis of salbutamol (4)
4. Describe in brief the biosynthesis, release, uptake and metabolism of
Norepinephrine.
5. Explain the SAR of sympathomimetics. Write the synthesis of salbutamol.
6. Classify sympathomimetic agents and describe their mode of action and
structural activity relationship.
7. a) Classify Para sympathomimetic agents with examples. b) Discuss the
structural activity relationship of cholinergic agonist.

5 MARKS
1. Describe the SAR of sympathomimetic agents.
2. Explain the biosynthesis, metabolism and physiological role of adrenergic
neurotransmitters.
3. Discuss the structural activity relationship of β blockers and outline the
synthesis of propranolol.
4. Classify sympathomimetic agents and outline the synthesis of salbutamol.
5. Write a note on cardio selective β1 blockers and write the structure and
medicinal uses of any two drugs.
6. Write a note on the different types of receptors meant for drug action.
7. Define beta-adrenergic blocking drugs with structural representation.
8. Summarize the SAR of beta-blockers.
9. Write a note on β blockers with α1 receptor antagonist activity with
chemical structure and its uses.
10. Discuss the chemistry and structural activity relationship of beta-adrenergic
blocking agents with examples.
11. Outline the synthesis and medicinal uses of (a) Propranolol (b) Tolazoline.*
12. Discuss the chemistry and structural activity relationship of alpha-adrenergic
blocking agents with examples.*
13. Write the structure, MOA & uses of Dopamine.
 14. Outline the synthesis and medicinal uses of (a) Phenylephrine (b)
Salbutamol.
15. Structure and uses of adrenaline and nor adrenaline.
16. Biosynthesis of catecholamines.

UNIT 3
10 MARKS
1. What are cholinergic agonists? Discuss the structural activity relationship
of cholinergic agonist. Outline the synthesis of Neostigmine.
2. Describe in brief the biosynthesis, release, uptake and metabolism of
acetylcholine.
3. Outline the synthesis and medicinal uses of (a) Ipratropium bromide (b)
Neostigmine (c) Carbachol (d) Dicyclomine hydrochloride.
4. a) Classify Para sympathomimetic agents with examples. b) Discuss the
structural activity relationship of cholinergic agonist.

5 MARKS
1. Write a note on synthetic cholinergic blocking agents.
2. Arrive biosynthesis and catabolism of acetyl choline*.
3. a) Explain the biosynthesis and catabolism of acetylcholine b) Explain
the muscarinic and nicotinic receptors and their distribution.
4. Classify cholinergic blocking agents. Outline the synthesis of
Dicyclomine hydrochloride.*
5. Write a note on cholinergic blocking agents.
6. Describe the chemistry of irreversible inhibitors of cholinesterase and
their mode of action.
7. Explain the structural considerations of solanaceous alkaloids.
8. Outline the synthesis of ipratropium bromide and mention its uses.
9. Classify parasympathomimetic agents and discuss the structural activity
relationship.
10. Describe about cholinesterase re-activators.
11. Classify parasympathomimetic agents with examples.
12. Write a note on cholinergic receptors and their distribution.
13. Describe in detail the structural activity relationship of cholinolytic
agents.*
UNIT 4
10 MARKS
1. a) What are sedative and hypnotics? Classify sedative and hypnotics. b)
Discuss the structural activity relationship of benzodiazepines and outline
the synthesis of diazepam.
2. a) Define and classify sedatives and hypnotics with suitable examples. (3) b)
Summarize the SAR of benzodiazepines. (3) c) Write the synthesis and use
of diazepam. (4)
3. a) Discuss the structural activity relationship of barbiturates. b) Sketch the
structure of Glutethimide and meprobamate and its medicinal uses.
4. Classify antipsychotics giving two examples with structures for each class.
Write the structural activity relationship and mode of action of
phenothiazine antipsychotics.
5. Classify Anti psychotic drugs. Write the synthesis of chlorpromazine.
6. Explain the SAR of Hydantoins with structures. Write the structure and uses
of succinimides.
7. a) Classify sedative and hypnotics with examples. b) Discuss the structural
activity relationship of Barbiturates.

5 MARKS
1. Present the SAR of phenothiazines*
2. Describe about anticonvulsants with appropriate chemical structures.
3. Write a short note on anti-psychotic drugs
4. Discuss the structural activity relationship of anticonvulsants* and outline
the synthesis and medicinal uses of ethosuximide.*
5. Explain the mechanism of action of Barbiturates and outline the synthesis of
barbital.
6. Outline the synthesis of carbamazepine and mention its uses and synthesis
7. Write a note on ultra short acting barbiturates and outline the synthesis of
Methohexital sodium.*
 8. Discuss the structural activity relationship of Phenotiazine.
9. a) Outline the synthesis of Chlorpromazine and its medicinal uses. b) Write
the structure of Trifluperazine and Thioridazine and mention their uses
10. Write a note on phenothiazines as antipsychotic agents.
11. What are anticonvulsants? Write the SAR of barbiturates.
12. Explain the formation of action potential and outline the synthesis of
phenytoin.*
13. Classify antipsychotics and write the structure and uses of (a)
Prochlorperazine maleate (b) Thiothixene.
14. Describe in detail the structural activity relationship of hydantoin class of
anticonvulsant drugs.
15. Describe in detail ring analogues of phenothiazine class of antipsychotic
drugs.
16. Classify sedatives and hypnotics. Outline the synthesis of diazepam.*
17. Write a brief note on benzodiazepines as anticonvulsant agent.
18. Structure and uses of lorazepam.
19. Describe in detail the structural activity relationship of barbiturates class of
sedatives and hypnotics.
20. Structures of a) Triclofos sodium b) paraldehyde c) Sodium salicylate d)
Droperidol e) Sulpier
21. Synthesis and uses of barbital sodium.
22. Write the structure and use of a) Phentolamine b) Pilocarpine c) Ephedrine
d) Paraldehyde e) Aspirin.

UNIT 5
10 MARKS
1. a) What are general anesthetics? Classify them with suitable examples. b)
Explain the mechanism of action of general anesthetic agents. Write the
synthesis of halothane.
2. Explain in detail the structural activity relationship of morphine and related
compounds.
3. a) Discuss the structural activity relationship of non narcotic anti
inflammatory agents. b) Outline the synthesis of Mefenamic acid and its
uses.
4. Explain the mechanism of action of general anesthetics and outline the
synthesis of ketamine hydrochloride and halothane.
5. Classify anti-inflammatory agents with examples for each class. Explain the
structural activity relationship and mode of action of anthranilic acid
derivatives.
6. Classify NSAIDS. Write the structure, uses and synthesis of Ibuprofen.
7. Define and classify narcotic analgesics. Elaborate the synthesis of
methadone HCI
8. Describe the SAR of morphine analogues. Write the synthesis of fentanyl
Citrate.

5 MARKS
1. Give synthesis and uses of Salbutamol and Ibuprofen.*
2. Write a note on narcotic analgesics.
3. Enumerate the facts about anti-inflammatory agents. Write the structure
and uses of : i) Mefenamic acid ii) Diclofenac.
4. Explain the mechanism of nonsteroidal anti-inflammatory agents and
outline the synthesis of Ibuprofen.
5. What are the general anesthetics? Classify general anesthetics with
examples.
6. What are narcotic analgesics? Classify narcotic analgesics and outline the
synthesis of fentanyl citrate.
7. Define general anesthetics with a mention on their mechanism of action.
Write the structure and uses and synthesis of i) Methohexital Sodium* ii)
Ketamine Hcl.*
8. What are NSAIDs? Write the synthesis of Ibuprofen.
9. Outline the synthesis of methadone hydrochloride and its uses.
10. Write a note on inhalation anesthetics with their structure and medicinal
uses.
11. a) What happens when dihydromorphinone is substituted with C-14
hydroxyl group. Sketch the resulting structure and its medicinal uses. b)
Sketch the structure of diphenoxylate and its uses.
12. Classify general anesthetics. Outline the synthesis of halothane.
13. Describe the synthesis and medicinal uses of (a) Fentanyl citrate (b)
Methadone hydrochloride.
14. Write a note on structural activity relationship of 3,5-pyrazolidine dione
derivatives used as anti-inflammatory agents.
15. Sketch the synthetic route and synthesis for Mefenamic acid.*
16. Discuss the structural activity relationship and mechanism of action of
morphine.
17. Define dissociative anesthetic**? Write the name, structure synthesis of
any one
18. Explain the structure, Mechanism of action and uses of Codeine.
19. Write a brief note on narcotic antagonists.
20. Structure and mechanism of action of pentazocine.
21. Write short notes on acetaminophen.
22. . Explain the mechanism of action of Narcotic antagonists and sketch the
structure of Nalorphine and Naloxone.