Medicinal Chemistry I: B.Pharmacy
Unit 1: Introduction to Medicinal Chemistry
1. What is meant by drugs? Explain the role of hydrogen bonding and Ionization and chelation in the biological activity of drugs with suitable examples.
2. List the various physicochemical properties that modulate biological activity and discuss the importance of partition coefficient in relation to biological activity.
3. Define drug metabolism. Why metabolism is also called detoxification reaction? Explain role of bio-isosterism in biological action.
4. What is meant by bioactivation? What are the main processes of drug absorption? Describe about simple diffusion and active transport.
5. List the main molecular targets of drugs. Discuss the specific role of ADME to enable a drug to reach the active site.
6. What is the difference between classical drug discover and rational drug discovery? Draw the chemical reaction of drug receptor interaction.
7. Write short notes on: Phase I and Phase II reactions.
1. Define general and local anaesthetics. Classify them with examples.
2. Define and classify local anesthetics. Explain SAR of local anesthetics with suitable examples.
3. Discuss the mechanism of action of Lignocaine
4. What are local anesthetics? How do they differ from general anesthetics? Write the structure, properties, metabolism, uses of lignocaine.
5. Write the chemical structure, properties, metabolism and mode of action of cocaine.
6. Outline the synthesis of the following drugs:
- Procaine from P-amino benzoic acid
- Lignocaine from 2, 6, xylidine
Unit 3: Drugs acting on Autonomic Nervous System
3.1. Adrenergic Neurotransmitters:
1. Define and classify the Adrenergic agents with examples. Write down the structure, properties and uses of Ephedrine.
2. What is meant by adrenergic drugs? Classify them on the basis of mode of action. Write the chemical structure, properties, metabolism and function of Dopamine.
3. Give the Structure, properties and uses of adrenaline.
4. Enumerate the synthetic scheme of Ephedrine from Benzene.
5. Why R-enantiomer.of noradrenaline is more active than S-enantiomer? Illustrate with examples.
6. Write the stereochemistry and biological effects of ephedrine.
7. Write SAR of sympathomimetic agents with suitable examples.
3.2 Adrenergic Antagonists
1. Classify adrenergic blockers with examples. Explain SAR Of Beta blockers with examples.
2. Define and classify adrenergic antagonists with examples. Discuss the SAR and uses of propranolol.
3. Write the structure, properties, synthesis and uses of propranolol.
4. What are alpha and beta adrenergic blocking drugs? Illustrate with suitable examples.
3.3 Cholinergic neurotransmitters:
1. Define and cholinergic agonists. Write the chemical structure, properties, mode of action and uses of Neostigmine.
2. Write mechanism of organophosphate poisoning and its recovery / mechanism with a suitable example.
3. Show MOA of irreversible cholinesterase inhibitors and cholinesterase reactivators.
4. Classify cholinergic drugs. Give the structure properties, uses and SAR of Acetylcholine.
5. Write the chemical structure, uses and metabolism Of Physostigmine
6. Show synthesis of neostigmine.
3.4 Cholinergic Blocking agents: SAR of cholinolytic agents
1. What do you mean by anticholinergic agents. Classify them with examples. Write the structure, properties, mechanism of action and uses of Atropine.
Unit 4: Drugs acting on Central Nervous System
4.1. Sedatives and Hypnotics:
1. Define sedative and hypnotic agents. Write structure, properties, MOA and uses of lorazepam.
2. Write Adverse effects of lorazepam.
3. Discuss the mechanism of action of Diazepam
4. Write notes on:
a. Metabolism of Benzodiazepines
5. Define and classify hypnotic agents with suitable examples. Write down structure, properties, uses and metabolism of Diazepam.
6. What are barbiturates? Classify them according to their duration of action with examples.
7. Define and classify CNS depressant drugs.
8. Write SAR of Barbiturates
9. Write SAR of Benzodizepines
10. Write the chemical structure, properties and clinical uses and synthesis of Phenobarbital.
4.2. Antipsychotics
1. Discuss about mechanism and uses of haloperidol
2. write SAR of Phenothiazine
4.3 Anticonvulsants
1. What are Benzodiazepines? Describe the properties, uses and mode of action of Phenytoin Sodium.
2. Write about MOA of Phenobarbitone
3. Write the chemical structures, properties, uses and metabolism of Valporic Acid
4. Write short notes on: Mode of action of anti-convulsant drugs
5. Write the chemical structure, uses and metabolism Of Carbamazipine
6. Enumerate the steps involved in the synthesis of following drugs.
a. Carbamazepine. B. Phenytoin sodium
7. Write SAR of hydantoins
8. Write short notes on Zolpidem
4.4 General anesthetics
1. Define and classify General anaesthetics with examples. Write down the chemical structure, properties and uses of Halothane.
2. Write chemical Structure, properties, metabolism and uses of one ultra-short acting Barbiturate.
3. What is meant by CNS depressants drug? Classify the general anaesthetics according to mode of administration with suitable examples.
4. Write short notes on:
a) Dissociative anaesthetic properties and dose of ketamine hydrochloride
5. Write notes on:
o Uses and MOA of Thiopental sodium
o Synthesis of Thiopental sodium from diethyl malonate
o Synthesis of ketamine
4.5. Narcotic and non-narcotic analgesics
1. What are Anti-tussive agents? Write the chemical structure, uses and MOA of Noscapine and Aspirin. 2. Define and classify narcotic and analgesic with suitable examples. Give the chemical structure, properties, and uses of morphine with example.
3. Write SAR of morphine.
4. What are Narcotic analgesics? Write the chemical structure, properties, uses and MOA of codeine.
5. Define and classify NSAIDs on the basic of chemical structure with examples.
6. Write the chemical structure, properties and MOA Of naloxone.
7. What axe NSAIDS? Write its adverse effects. Write the chemical structure, properties, uses and synthesis of mefenamic acid from o-chloro benzoic acid.
8. Outline the synthesis and uses of: Ibuprofen
9. Differentiate between steroidal anti-inflammatory drugs and non-steroidal anti- inflammatory drugs with examples.
10. Write the chemical structure, properties, uses, synthesis, adverse effect and mode of action of paracetamol and diclofenac.
11. Enumerate the steps involved in synthesis of: Ibuprofen from isobutyl benzene
12. SAR of Morphine analogue.
Unit 5: Prostaglandin and other eicosanoids
1. What is meant by Eicosonoids? Write the chemical structure and uses of Prostaglandine F2a, PGEI and Oxytocin.
2. Write shorts notes on Prostaglandin
3. MOA of oxytocin 2. Write the chemical structure, Dose and uses of:
a. Prostaglandin F2a
b. Oxytocin
Unit 6: Cardiovascular agents
1. Classify antihyperlipidemic agents with examples. Write structure, MOA and uses of nitroglycerine and warfarin.
2. Discuss about mechanism of action and uses of: Frusemide
3. Shorts notes on Losartan
Unit 7: Drugs acting on endocrine system
1. Write in brief about stereochemistry and metabolism of steroids. Write structure, MOA and uses of mifepristone and sildenafil.
2. Discuss MOA Sildenafd Citrate.
3. Mention the therapeutic classification of steroids. “stereo chemistry of steroids rings markedly affect biological activity.' Justify this statement with the discussion Of stereochemistry of steroids.
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