UNIQUE SERIES AKTU Syllabus
BP402T

Medicinal Chemistry (Theory)

L-T-P3-0-0 Credits3 Session2026-27 TypeTheory
Appears in 1 semester

B.Pharm · Sem 4 (Core)

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Syllabus

5 units · 45 lecture hours
Unit1

Unit 1

7 hrs

Fundamentals of Medicinal Chemistry Introduction: History and scope of medicinal chemistry Physicochemical properties in relation to biological action: Ionization, solubility, partition coefficient, hydrogen bonding, Chelation, Bioisosterism and protein binding Drug metabolism: Phase I & II reactions

Unit2

Unit 2: Drugs Acting on the Autonomic Nervous System

15 hrs
  • Adrenergic or Sympathomimetic agents: Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline, Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine, Metaraminol.
  • Anti-adrenergic or Sympatholytic agents: Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Propranolol*, Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetalol, Carvedilol. SAR of beta adrenergic blockers.
  • Cholinergic or Parasympathomimetic agents: Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine, Physostigmine, Neostigmine, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion. Pralidoxime chloride.
  • Anti-Cholinergic or Parasympatholytic agents: Atropine, Hyoscyamine, Scopolamine, Homatropine, Ipratropium*, Tropicamide, Cyclopentolate, Clidinium Glycopyrrolate, Dicyclomine*, Methantheline, Propantheline, Benztropine mesylate, Orphenadrine, Biperidine, Procyclidine, Tridihexethyl, Isopropamide, Ethopropazine, SAR of cholinergic blockers.
  • Local anesthetic agents: Cocaine, Hexylcaine, Meprylcaine, Cyclomethycaine, Piperocaine. Benzocaine, Butamben, Procaine*, Butacaine, Propoxycaine, Tetracaine, Benoxinate, Lignocaine, Mepivacaine, Prilocaine, Etidocaine, Phenacaine, Diperodon, Dibucaine.* SAR of Local anesthetics.
Unit3

Unit 3: Drugs Acting on the Cardiovascular System

9 hrs
  • Anti-anginals: Amyl nitrite, Nitroglycerin, Pentaerythritol, Isosorbide dinitrite*, Dipyridamole, Verapamil, Bepridil hydrochloride, Diltiazem, Nifedipine, Amlodipine, Felodipine, Nicardipine, Nimodipine.
  • Anti-hypertensives: Timolol, Captopril, Lisinopril, Enalapril, Benazepril, Quinapril, Methyldopate,* Clonidine, Guanethidine, Guanabenz, Sodium nitroprusside, Diazoxide, Minoxidil, Reserpine, Hydralazine.
  • Drugs to treat Congestive Heart Failure (CHF): Digoxin, Digitoxin, Nesiritide, Bosentan,Tezosentan.
  • Anti-arrhythmics (Class I IV): Quinidine sulphate, Procainamide, Disopyramide*, Phenytoin, Lidocaine, Tocainide, Mexiletine, Lorcainide, Amiodarone, Sotalol.
Unit4

Unit 4: Drugs acting on blood and Renal System

6 hrs
  • Antihyperlipidemic Agents: Fenofibrate*, Lovastatin, Cholesteramine and Cholestipol
  • Coagulants and Anti-Coagulants: Menadione, Acetomenadione, Warfarin, Anisindione, clopidogrel.
  • Diuretics: Acetazolamide*, Methazolamide, Dichlorphenamide, Chlorthiazide, Hydrochlorothiazide, Hydroflumethiazide, Cyclothiazide, Furosemide*, Bumetanide, Ethacrynic acid, Spironolactone, Triamterene, Amiloride. Mannitol. SAR of Thiazides.
Unit5

Unit 5: Autacoids and related drugs

8 hrs
  • Antihistamines a. H1 antagonists: Diphenhydramine hydrochloride*, Dimenhydrinate, Doxylamines, Clemastine, Diphenylphyraline, Tripelenamine, Chlorcyclizine, Meclizine, Buclizine, Chlorpheniramine, Triprolidine, Phenindamine, Promethazine*, Trimeprazine, Cyproheptadine, Azatidine, Astemizole, Loratadine, Cetirizine, Levocetrizine Cromolyn. b. H2-antagonists: Cimetidine*, Famotidine, Ranitidine.
  • Gastric Proton pump inhibitors: Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), Antipyretics: Sodium salicylate, Aspirin, Diflunisal, Mefenamic acid*, Niflumic acid, Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepirac, Diclofenac, Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone, Celecoxib, Etoricoxib, SAR of representative agents by class.
Course Objectives6 points
  • The objectives of this course are to:
  • Develop a comprehensive understanding of the fundamental principles of medicinal chemistry, including physicochemical properties, drug metabolism, and prodrug concepts.
  • Classify and describe the chemical structures, therapeutic uses, and structure activity relationships of drugs acting on the autonomic and cardiovascular systems.
  • Apply the principles of structure activity relationships (SAR) to explain and predict the pharmacological activity.
  • Understand the synthetic pathways of drugs, emphasizing important reaction steps and chemical transformations.
  • Analyze the relationship between drug structure and pharmacological activity in relation to therapeutic efficacy and safety.
Course Outcomes (COs)5 outcomes

After completion of the course student will be able to:

  1. CO1Relate the physicochemical properties of drug molecules to their biological activity and pharmacokinetic behavior.
  2. CO2Categorize drugs affecting the autonomic nervous system and predict their therapeutic outcomes.
  3. CO3Analyze and interpret the structure-activity relationships of selected drug classes (e.g., beta-blockers, local anesthetics, thiazide diuretics, NSAIDs) to optimize drug design.
  4. CO4Outline the synthetic routes of selected drugs, identifying key intermediates and reactions involved in their preparation.
  5. CO5Correlate the chemical structure of drugs with their therapeutic uses and potential adverse effects. Apply the knowledge of medicinal chemistry principles to understand and potentially contribute to the drug discovery and development process.
Text Books & References11 books

Recommended References (Preferably latest editions):

  1. Lemke, T. L., Williams, D. A. and Roche, V. F. Chemistry. Lippincott Williams & Wilkins.
  2. Beale, J. M., Thomas, J. T. and Duckett, M. H. Organic Medicinal and Pharmaceutical Chemistry. Lippincott Williams & Wilkins.
  3. Abraham, D. J. and Griffin, J. L. Discovery. Wiley.
  4. Patrick, G. L. An Introduction to Medicinal Chemistry. Oxford University Press.
  5. Kar, A. Medicinal Chemistry. New Age International.
  6. Li, J. J. and Welch, W. M. Modern Drug Synthesis. Wiley.
  7. Lednicer, D. The Organic Chemistry of Drug Synthesis. Wiley.
  8. Furniss, B. S., Hannaford, A. J., Smith, P. W. G. and Tatchell, A. R.

Textbook

  1. of Practical Organic Chemistry. Pearson Education.
  2. Brunton, L., Hilal-Dandan, R. and Knollmann, B. Pharmacological Basis of Therapeutics. McGraw-Hill Education.
  3. Wilkins. Course Title Course Type

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Official AKTU syllabus

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Official AKTU syllabus PDF ↗