Medicinal Chemistry I-(Theory)
Teacher
Dr. Gopal Krishna Padhy
Category
Core Courses
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Code(Credit) : BPHT2202 (4-0-0)
Course Objectives
- To expose students towards different chemical classes of drugs and their pharmacological activity.
- To develop the linkage between organic molecules and their transformation to the drug molecule
- To explain the mechanisms of action for representative drug classes.
- To explain the relationship between drug’s chemical structure and it’s therapeutic properties.
- To discuss the metabolic pathways, adverse effect and therapeutic indications of drug molecules.
Course Outcomes
| CO | Statement | Mapping with POs |
| CO-1 | Understand the importance of drug design and different techniques of drug design. | PO1, PO2, PO5 |
| CO-2 | Understand the chemistry of drugs with respect to their biological activity. | PO1, PO2, PO5 |
| CO-3 | Know the metabolism, adverse effects and therapeutic value of drugs. | PO1, PO2, PO5 |
| CO-4 | To develop entrepreneurship qualities that support growth of pharmaceutical | PO1, PO2, PO5 |
| CO-5 | Implementing the knowledge to determine Structure, nomenclature, metabolism and uses of Various Antibiotics., Chemotherapeutic agents. | PO1, PO2, PO5 |
Course Syllabus
Module- 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.
Module- 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
Module- 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.
Module- 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
Miscelleneous:
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
Module- 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.
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. 1to 5.
9. Indian Pharmacopoeia.
10. Text book of practical organic chemistry- A.I.Vogel.
Session Plan
Session 39
Our Main Teachers
He obtained his M.Pharm. degree in Pharmaceutical chemistry from Poona College of Pharmacy, Bharati Vidyapeeth University, Pune in 2007. He had carried out his Ph.D. work under joint supervision of Dr. Ajaya Kumar behera and Dr. Jagadeesh Panda in Sambalpur University. He worked as an assistant professor in Maharajah’s College of Pharmacy, Phool baugh, Vizianagaram, AP from Oct. 2007-Nov. 2019 (12 years). Currently he is working as an associate professor in School of Pharmacy, CUTM, Rayagada since Dec. 2019.