Medicinal Chemistry Course Overview
Medicinal Chemistry Course Overview
77
BP401T PHARMACEUTICAL ORGANIC CHEMISTRY –III (Theory)
3 L + 1T / Week
Scope: This subject imparts knowledge on stereo-chemical aspects of organic
compoundsand organic reactions, important named reactions, chemistry of important hetero
cyclic compounds. It also emphasizes on medicinal and other uses of organic compounds.
Objectives: At the end of the course, the student shall be able to:
1. understand the methods of preparation and properties of organic compounds
2. explain the stereo chemical aspects of organic compounds and stereo chemical reactions
3. know the medicinal uses and other applications of organic compounds
Sr. Content Hours
No. Note: To emphasize on definition, types, mechanisms, examples,
uses/applications
1 UNIT I 10
Stereo isomerism
Optical isomerism –
i. Optical activity, enantiomerism, diastereoisomerism, meso compounds
ii. Elements of symmetry, chiral and achiral molecules
iii. DL system of nomenclature of optical isomers, sequence rules, RS
system of nomenclature of optical isomers
iv. Reactions of chiral molecules
v. Racemic modification and resolution of racemic mixture.
vi. Asymmetric synthesis: partial and absolute
2 UNIT II 10
Geometrical isomerism
i. Nomenclature of geometrical isomers (Cis Trans, EZ, Syn Anti systems)
ii. Methods of determination of configuration of geometrical isomers.
iii. Conformational isomerism in Ethane, n-Butane and Cyclohexane.
iv. Stereo isomerism in biphenyl compounds (Atropisomerism) and
conditions for optical activity.
v. Stereospecific and stereoselective reactions
3 UNIT III - Heterocyclic compounds: 10
Heterocyclic compounds:
Nomenclature and classification
Synthesis, reactions and medicinal uses of following compounds/derivatives
Pyrrole, Furan, and Thiophene
Relative aromaticity and reactivity of Pyrrole, Furan and Thiophene
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4 UNIT IV 08
Synthesis, reactions and medicinal uses of following compounds/derivatives
Pyrazole, Imidazole, Oxazole and Thiazole.
Pyridine, Quinoline, Isoquinoline, Acridine and Indole. Basicity of pyridine
Synthesis and medicinal uses of Pyrimidine, Purine, azepines and their
derivatives
5 UNIT V - Reactions of synthetic importance 07
5.1 Metal hydride reduction (NaBH4 and LiAlH4), Clemmensen reduction, 2
Birch reduction, Wolff Kishner reduction
Total 45
79
BP402T MEDICINAL CHEMISTRY – I (Theory) 3 L + 1T / Week
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:
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Xylometazoline
Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine,
Propylhexedrine.
Agents with mixed mechanism: Ephedrine, Metaraminol.
2.3 Adrenergic Antagonists: 4
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.
3 UNIT III - Cholinergic neurotranimitters 10
3.1 Biosynthesis and catabolism of acetylcholine. 2
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution
3.2 Parasympathomimetic agents: SAR of Parasympathomimetic agents 4
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.
3.3 Cholinergic Blocking agents: SAR of cholinolytic agents 4
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.
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Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital
Miscelleneous:
Amides and imides:Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.
4.2 Antipsychotics 3
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.
4.3 Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant 2
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
5 UNIT V- Drugs acting on Central Nervous System 07
5.1 General anesthetics: 3
Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane,
Sevoflurane, Isoflurane, Desflurane.
Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal
sodium, Thiopental sodium.
Dissociative anesthetics: Ketamine hydrochloride.*
5.2 Narcotic and non-narcotic analgesics 2
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.
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Narcotic antagonists: Nalorphine hydrochloride, Levallorphan
tartarate, Naloxone hydrochloride
5.3 Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid*, 2
Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac,
Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen,
Antipyrine, Phenylbutazone
Total 45
83
BP403T PHYSICAL PHARMACEUTICS-II (Theory) 3 L + 1T / Week
Scope: The course deals with the various physical and physicochemical properties,
andprinciples involved in dosage forms/formulations. Theory and practical components of the
subject help the student to get a better insight into various areas of formulation research and
development, and stability studies of pharmaceutical dosage forms.
Objectives: Upon the completion of the course student shall be able to:
1. Understand various physicochemical properties of drug molecules in the designing the
dosage forms
2. Know the principles of chemical kinetics & to use them for stability testing and
determination of expiry date of formulations
3. Demonstrate use of physicochemical properties in the formulation development and
evaluation of dosage forms
Sr. Content Hours
No.
1 UNIT I 7
Colloidal dispersions: Classification of dispersed systems & their general
characteristics, size & shapes of colloidal particles, classification of colloids
& comparative account of their general properties. Optical, kinetic &
electrical properties. Effect of electrolytes, coacervation, peptization&
protective action.
2 UNIT II 10
2.1 Rheology: Newtonian systems, law of flow, kinematic viscosity, effect of 7
temperature, non-Newtonian systems, pseudoplastic, dilatants, plastic,
thixotropy, thixotropy in formulation, determination of viscosity, capillary,
falling Sphere, rotational viscometers
2.2 Deformation of solids: Plastic and elastic deformation, Heckel equation, 3
Stress, Strain, Elastic Modulus
3 UNIT III - Coarse dispersion 10
3.1 Suspension, interfacial properties of suspended particles, settling in 7
suspensions, formulation of suspensions. Emulsions and theories of
emulsification, microemulsion and multiple emulsions;
3.2 Physical stability of emulsions, preservation of emulsions, rheological 3
properties of emulsions, phase equilibria and emulsion formulation.
4 UNIT IV 8
Micromeretics: Particle size and distribution, mean particle size, number
and weight distribution, particle number, methods for determining particle
size by different methods, counting and separation method, particle shape,
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specific surface, methods for determining surface area, permeability,
adsorption, derived properties of powders, porosity, packing arrangement,
densities, bulkiness & flow properties.
5 UNIT V 10
5.1 Drug stability: Reaction kinetics: zero, pseudo-zero, first & second order,
units of basic rate constants, determination of reaction order. Physical and
chemical factors influencing the chemical degradation of pharmaceutical
product: temperature, solvent, ionic strength, dielectric constant, specific &
general acid base catalysis, Simple numerical problems. Stabilization of
medicinal agents against common reactions like hydrolysis & oxidation.
Accelerated stability testing in expiration dating of pharmaceutical dosage
forms. Photolytic degradation and its prevention
Total 45
85
BP404T PHARMACOLOGY-I (Theory) 3 L + 1T / Week
Scope: The main purpose of the subject is to understand what drugs do to the livingorganisms
and how their effects can be applied to therapeutics. The subject covers the information about
the drugs like, mechanism of action, physiological and biochemical effects
(pharmacodynamics) as well as absorption, distribution, metabolism and excretion
(pharmacokinetics) along with the adverse effects, clinical uses, interactions, doses,
contraindications and routes of administration of different classes of drugs.
Objectives: Upon completion of this course the student should be able to
1. Understand the pharmacological actions of different categories of drugs
2. Explain the mechanism of drug action at organ system/sub cellular/ macromolecular
levels.
3. Apply the basic pharmacological knowledge in the prevention and treatment of various
diseases.
4. Observe the effect of drugs on animals by simulated experiments
5. Appreciate correlation of pharmacology with other bio medical sciences
Sr. No. Content Hours
1 UNIT I - General Pharmacology 8
1.1 Introduction to Pharmacology- Definition, historical landmarks and scope 4
of pharmacology, nature and source of drugs, essential drugs concept and
routes of drug administration, Agonists, antagonists( competitive and non-
competitive), spare receptors, addiction, tolerance, dependence,
tachyphylaxis, idiosyncrasy, allergy
1.2 Pharmacokinetics- Membrane transport, absorption, distribution, 4
metabolism and excretion of drugs .Enzyme induction, enzyme inhibition,
kinetics of elimination
2 UNIT II - General Pharmacology 12
2.1 Pharmacodynamics- Principles and mechanisms of drug action. Receptor 6
theories and classification of receptors, regulation of receptors. drug
receptors interactions signal transduction mechanisms, G-protein–coupled
receptors, ion channel receptor, transmembrane enzyme linked receptors,
transmembrane JAK-STAT binding receptor and receptors that regulate
transcription factors, dose response relationship, therapeutic index,
combined effects of drugs and factors modifying drug action.
2.2 Adverse drug reactions. 2
2.3 Drug interactions (pharmacokinetic and pharmacodynamic) 2
2.4 Drug discovery and clinical evaluation of new drugs -Drug discovery phase, 2
preclinical evaluation phase, clinical trial phase, phases of clinical trials and
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pharmacovigilance
3 UNIT III –Pharmacology of peripheral nervous system 10
3.1 Organization and function of ANS, Neurohumoral transmission,co- 1
transmission and classification of neurotransmitters
3.2 Parasympathomimetics, Parasympatholytics, Sympathomimetics, 3
sympatholytics
3.3 Neuromuscular blocking agents and skeletal muscle relaxants (peripheral). 2
3.4 Local anesthetic agents 3
3.5 Drugs used in myasthenia gravis and glaucoma 1
4 UNIT IV - Pharmacology of central nervous system 08
4.1 Neurohumoral transmission in the [Link] emphasis on importance of 1
various neurotransmitters like with GABA, Glutamate, Glycine, serotonin,
dopamine.
4.2 General anesthetics and pre-anesthetics. 2
4.3 Sedatives, hypnotics and centrally acting muscle relaxants 2
4.4 Anti-epileptics 2
4.5 Alcohols and disulfiram 1
5 UNIT V - Pharmacology of central nervous system 07
5.1 Psychopharmacological agents: Antipsychotics, antidepressants, anti- 2
anxiety agents, anti-manics and hallucinogens
5.2 Drugs used in Parkinsons disease and Alzheimer‘s disease. 1
5.3 CNS stimulants and nootropics 1
5.4 Opioid analgesics and antagonists 2
5.5 Drug addiction, drug abuse, tolerance and dependence. 1
Total 45
Reference Books (Latest Editions to be adopted)
1. Rang H. P., Dale M. M., Ritter J. M., Flower R. J., Rang and Dale‘s
Pharmacology,.Churchil Livingstone Elsevier
2. Katzung B. G., Masters S. B., Trevor A. J., Basic and clinical pharmacology, Tata Mc
Graw-Hill
3. Goodman and Gilman‘s, The Pharmacological Basis of Therapeutics
4. Marry Anne K. K., Lloyd Yee Y., Brian K. A., Robbin L.C., Joseph G. B., Wayne A. K.,
Bradley R.W., Applied Therapeutics, The Clinical use of Drugs, The Point Lippincott
Williams & Wilkins
5. Mycek M.J, Gelnet S.B and Perper M.M. Lippincott‘s Illustrated Reviews- Pharmacology
6. [Link]. Essentials of Medical Pharmacology, JAYPEE Brothers Medical Publishers
(P) Ltd, New Delhi.
7. Sharma H. L., Sharma K. K., Principles of Pharmacology, Paras medical publisher
87
8. Modern Pharmacology with clinical Applications, by Charles [Link]& Robert,
9. Ghosh MN. Fundamentals of Experimental Pharmacology. Hilton & Company, Kolkata.
10. Kulkarni SK. Handbook of experimental pharmacology. VallabhPrakashan
88
BP405T PHARMACOGNOSY AND PHYTOCHEMISTRY I (Theory)
3 L + 1T / Week
Scope: The subject involves the fundamentals of Pharmacognosy like scope, classification of
crude drugs, their identification and evaluation, phytochemicals present in them and their
medicinal properties.
Total 45
90
3. Text Book of Pharmacognosy by T.E. Wallis
4. Mohammad Ali. Pharmacognosy and Phytochemistry, CBS Publishers & Distribution,
New Delhi.
5. Text book of Pharmacognosy by C.K. Kokate, Purohit, Gokhlae (2007), 37th Edition,
Nirali Prakashan, New Delhi.
6. Herbal drug industry by R.D. Choudhary (1996), Ist Edn, Eastern Publisher, New Delhi.
7. Essentials of Pharmacognosy, [Link], IInd edition, Birla publications, New Delhi,
2007
8. Practical Pharmacognosy: C.K. Kokate, Purohit, Gokhlae
9. Anatomy of Crude Drugs by M.A. Iyengar
91
BP406P MEDICINAL CHEMISTRY – I (Practical) 3 L + 1T / Week
92
BP407P PHYSICAL PHARMACEUTICS- II (Practical) 3 L + 1T / Week
93
7. Study of effect of hepatic microsomal enzyme inducers on the phenobarbitone sleeping
time in mice.
8. Effect of drugs on ciliary motility of frog oesophagus
9. Effect of drugs on rabbit eye.
10. Effects of skeletal muscle relaxants using rota-rod apparatus.
11. Effect of drugs on locomotor activity using actophotometer.
12. Anticonvulsant effect of drugs by MES and PTZ method.
13. Study of stereotype and anti-catatonic activity of drugs on rats/mice.
14. Study of anxiolytic activity of drugs using rats/mice.
15. Study of local anesthetics by different methods
Note: All laboratory techniques and animal experiments are demonstrated by simulated
experiments by softwares and videos
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BP409P PHARMACOGNOSY AND PHYTOCHEMISTRY I (Practical)
4 Hours/Week
1. Analysis of crude drugs by chemical tests: (i)Tragaccanth (ii) Acacia (iii)Agar (iv) Gelatin
(v) starch (vi) Honey (vii) Castor oil
2. Determination of stomatal number and index
3. Determination of vein islet number, vein islet termination and paliside ratio.
4. Determination of size of starch grains, calcium oxalate crystals by eye piece micrometer
5. Determination of Fiber length and width
6. Determination of number of starch grains by Lycopodium spore method
7. Determination of Ash value
8. Determination of Extractive values of crude drugs
9. Determination of moisture content of crude drugs
10. Determination of swelling index and foaming
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