Medicinal Chemistry I – B. Pharma 4th Semester Notes Pdf

Medicinal Chemistry I – B. Pharma 4th Semester Notes Pdf

medicinal chemistry b pharma 4th semester notes

Scope: This subject is designed to impart fundamental knowledge on the structure, chemistry and therapeutic value of drugs. The subject emphasizes on structure activity relationships of drugs, importance of physicochemical properties and metabolism of drugs. The syllabus also emphasizes on chemical synthesis of important drugs under each class.

Objectives: Upon completion of the course the student shall be able to

1.  Understand the chemistry of drugs with respect to their pharmacological activity

2.  Understand the drug metabolic pathways, adverse effect and therapeutic value of drugs

3.  Know the Structural Activity Relationship (SAR) of different class of drugs

4.  Write the chemical synthesis of some drugs

Course Content:

Study of the development of the following classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted (*)

Medicinal Chemistry I UNIT- I

Introduction to Medicinal Chemistry

History and development of medicinal chemistry

Physicochemical properties in relation to biological action

Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.

Drug metabolism

Drug metabolism principles- Phase I and Phase II.

Factors affecting drug metabolism including stereo chemical aspects.

Medicinal Chemistry I UNIT- II

Drugs acting on Autonomic Nervous System

Adrenergic Neurotransmitters:

Biosynthesis and catabolism of catecholamine.

Adrenergic receptors (Alpha & Beta) and their distribution.

Sympathomimetic agents: SAR of Sympathomimetic agents

Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.

Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.

Agents with mixed mechanism: Ephedrine, Metaraminol.

Adrenergic Antagonists:

Alpha adrenergic blockers:  Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide.

Beta adrenergic blockers: SAR of beta blockers, Propranolol*, Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol, Carvedilol.

Medicinal Chemistry I UNIT-III

Cholinergic neurotransmitters:

Biosynthesis and catabolism of acetylcholine.

Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.

Parasympathomimetic agents: SAR of Parasympathomimetic agents

Direct acting agents:  Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine.

Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible): Physostigmine, Neostigmine*, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion.

Cholinesterase reactivator: Pralidoxime chloride.

Cholinergic Blocking agents: SAR of cholinolytic agents

Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide*.

Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate hydrochloride, Clidinium bromide, Dicyclomine hydrochloride*, Glycopyrrolate, Methantheline bromide, Propantheline bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride, Procyclidine hydrochloride*, Tridihexethyl chloride,  Isopropamide iodide, Ethopropazine hydrochloride.

Medicinal Chemistry I UNIT- IV

Drugs acting on Central Nervous System

A. Sedatives and Hypnotics:

Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam*, Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem

Barbiturtes: SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital


Amides & imides: Glutethmide.

Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol. Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.

B. Antipsychotics

Phenothiazeines: SAR of Phenothiazeines – Promazine hydrochloride, Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine hydrochloride, Prochlorperazine maleate, Trifluoperazine hydrochloride.

Ring Analogues of Phenothiazeines: Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine.

Fluro buterophenones: Haloperidol, Droperidol, Risperidone.

Beta amino ketones: Molindone hydrochloride.

Benzamides: Sulpieride.

C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action

Barbiturates: Phenobarbitone, Methabarbital. Hydantoins: Phenytoin*, Mephenytoin, Ethotoin Oxazolidine diones: Trimethadione, Paramethadione Succinimides: Phensuximide, Methsuximide, Ethosuximide* Urea and monoacylureas: Phenacemide, Carbamazepine* Benzodiazepines: Clonazepam

Miscellaneous: Primidone, Valproic acid, Gabapentin, Felbamate

Medicinal Chemistry I UNIT – V

Drugs acting on Central Nervous System

General anesthetics:

Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane.

Ultra short acting barbitutrates: Methohexital sodium*,  Thiamylal sodium, Thiopental sodium.

Dissociative anesthetics: Ketamine hydrochloride.*

Narcotic and non-narcotic analgesics

Morphine and related drugs: SAR of Morphine analogues, Morphine sulphate, Codeine, Meperidine hydrochloride, Anilerdine hydrochloride, Diphenoxylate hydrochloride, Loperamide hydrochloride, Fentanyl citrate*, Methadone hydrochloride*, Propoxyphene hydrochloride, Pentazocine, Levorphanol tartarate.

Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartarate, Naloxone hydrochloride.

Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate, Indomethacin, Sulindac, Tolmetin,  Zomepriac, Diclofenac, Ketorolac,  Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone.


I Preparation of drugs/ intermediates

1. 1,3-pyrazole 

2. 1,3-oxazole   

3. Benzimidazole             

4. Benztriazole 

5. 2,3- diphenyl quinoxaline       

6. Benzocaine   

7. Phenytoin     

8. Phenothiazine             

9. Barbiturate   

II Assay of drugs

1. Chlorpromazine          

2. Phenobarbitone         

3. Atropine        

4. Ibuprofen      

5. Aspirin            

6. Furosemide  

III Determination of Partition coefficient for any two drugs       

Recommended Books (Latest Editions)

1. Wilson and Giswold’s Organic medicinal and Pharmaceutical Chemistry.

2. Foye’s Principles of Medicinal Chemistry.

3. Burger’s Medicinal Chemistry, Vol I to IV.

4. Introduction to principles of drug design- Smith and Williams.

5. Remington’s Pharmaceutical Sciences.

6. Martindale’s extra pharmacopoeia.

7. Organic Chemistry by I.L. Finar, Vol. II.

8. The Organic Chemistry of Drug Synthesis by Lednicer, Vol. 1-5.

9. Indian Pharmacopoeia.

10. Text book of practical organic chemistry- A.I.Vogel.

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