department of chemistry dr. harisingh gour vishwavidyalaya ... - pch... · dr. harisingh gour...

46

Department of Chemistry

Dr. Harisingh Gour Vishwavidyalaya, Sagar (M.P.)

B.Sc. Pharmaceutical Chemistry

Semester I

Semester I

Course Code Course Name Credits

PCH-C-111 Gen Topics for Pharma Chemistry-I 2

PCH-C-112 Pharmaceutical Analysis-I 2

PCH-C-113 Laboratory Course 2

47

PCH- C - 111

B.Sc. Pharmaceutical Chemistry- Semester I

Paper-I : General topics for Pharmaceutical Chemistry-I

Credits : 2 30 Hrs

1. Diseases and Prevention, First Aid : Concepts of health and diseases, disease agents and

prevention of diseases, emergency treatment of shock, snake bites, burns, poisoning,

fracture and resurrection methods

6

2. Inorganic Radio-Pharmaceuticals: Nuclear reactions, nomenclature methods of

obtaining, measurement of activity, clinical applications and dosage, nuclear hazards and its

precautions.

6

3. Surface and Interfacial Phenomenon: Surface and interfacial tensions, surface free

energy, measurement of surface and interfacial tensions. 6

4. Viscosity and Rheology: Newtonian systems: Law of flow, kinematics viscosity effect of

temperature, Non-Newtonian systems, pseudoplastic, dilatent and plastic flow, thixotropy,

measurement of thixotropy, thixotropy in formulation.

6

5. Micrometrics and Powder Rheology : Particle size and distribution, average particle size,

number and weight distribution, particle number, methods for determining particle volume,

optical volume, optical microscopy, sieving, sedimentation, particle shape, specific surface,

methods for determining surface area, derived properties of powders: porosity, packing

arrangement, densities, bulkiness and flow properties

6

Course Coordinator Dr. Ratnesh Das

PCH –C-112

B.Sc. Pharmaceutical Chemistry - Semester - I

Paper-II : Pharmaceutical Analysis-I Credits : 2 30 Hrs

1. Aqueous Acid-Base Titrations: Acid-Base Equilibria, Acid-Base Titrations. 4

2. Non-Aqueous Acid-Base Titrations: Dissociating and non-dissociating solvents, dielectric

constant, ionisation and dissociation, determination of acids and bases. 6

3. Precipitation Titrations: Solubility, solubility product, effect of pH on solubility of salts,

Vohlard determination of chloride. 4

4. Complexometric Titrations: EDTA complexes, titration with EDTA, determination of

total hardness in water. 4

5. Oxidation-Reduction Titrations: Half reactions, balancing equations, redox equivalent

weights, titration with permanganate, iodometric titrations, titrations with ceric salts,

iodimetric titrations, biological redox systems

4

6. Potentiometric Technique of Analysis : Basic principle, electrode potential, standard

electrode potential, reference, indicator and reversible electrodes, potentiometric titrations,

potentiometric determination of equilibrium constants. Kinetic Methods of Analysis: Rates of chemical reactions, enzymes, determining reaction

rates, fast reactions, kinetic methods to the enzyme.

4

4


48

PCH- C - 113

B.Sc. Pharmaceutical Chemistry : Semester - I

Laboratory Course Credits : 2

• Detection of association of phenylacetic acid in solution.

• Determination of critical micelle concentration by refractometry.

• Determination of the loss on drying.

• Estimation of Cu in a given Cu alloy by iodometric titration.

• Determination of Ash values including Acid-insoluble ash, water soluble ash.

• Determination of pH of natural and biological samples.

• pH metric titrations.

• Oxidation-Reduction titration.

• Determination of sulphate in lactic acid.

• Determination of Acid value of fixed oil.


49


Dr. Hari Singh Gour Vishwavidyalaya, Sagar (M.P.)


Semester II

Semester II


PCH-C-211 Gen Topics of Pharma Chemistry-II 2

PCH-C-212 Pharmaceutical Analysis-II 2


50

PCH-C-211

B.Sc. Pharmaceutical Chemistry - Semester II

Paper-I : General topics for Pharmaceutical Chemistry-II Credits : 2 30 Hrs

1. Nutrition : Classification of food requirements, balanced diet, nutritional deficiency

disorders and their treatment and prevention. 3

2. Demography and Family Planning : Demography cycle, family planning, various

contraceptive methods, medical termination of pregnancy. 4

3. Communicable Diseases : Brief outline of communicable diseases, their causative agents,

mode of transmission and prevention. 4

4. Industrial Hazards and Safety Measures : Mechanical, chemical, electrical, fire and dust

hazards, safety requirements, legal requirements, industrial dermatitis. 5

5. Compaction and Compression: Adhesion and cohesion of particles strength of granules,

factors affecting strength of tablets, physics of tablet compression. 3

6. Gravimetric Methods of Analysis: Principle of gravimetry, co-precipitation, post

precipitation, gravimetric calculations (chemical stoichiometry), application of gravimetric

methods in quantitative analysis.

6

7. Electrogravimetric Methods: Electrogravimetric and Coulometric methods of analysis,

coulometric titration of chloride in biological fluids. 5


PCH – C - 212

B.Sc. Pharmaceutical Chemistry - Semester II

Paper-II : Pharmaceutical Analysis-II Credits : 2 30 Hrs

1. Polarography : Basic principle of DC polarography, polarograms, polarographic waves,

residual current, diffusion current, half wave potential, DP polarography, qualitative and

quantitative polarographic determination of electroactive species, polarographic determination

of Ascorbic acid and concentration of Vitamin C in fruit juice, polarographic determination of

metal ions in synthetic and natural origin samples

10

2. Chromatographic Techniques : Principles of Chromatographic separation;, terminology –

elution, eluent, front ratio, Rf, solvent system, Classification of chromatographic techniques-

adsorption, partition, size exclusion, ion exchange, solvent extraction, electrophoresis;

chromatographic classification on the basis of stationary and mobile phase, Column

chromatography, types , factors affecting chromatographic separation, applications of

chromatographic analysis

10

3. Ion Exchange Chromatography : Basic principles - anion and cation exchangers exchange

capacity, applications of ion exchange technique : determination of anions (in drinking water,

in ethanol and spirits, phosphoric acid in cola drinks, organic acids in wines, in waste water,

fluoride in toothpaste, in brown and white sugar etc), determination of cations (in drinking and

mineral water, in wine, cosmetics), corrosion protection : determination of ethanolamine and

alkali metals

10


51

PCH-C- 213

B.Sc. Pharmaceutical Chemistry -Semester II

Laboratory Course Credits : 2

1. Determination of the percentage of C6H5COONa.

2. Determination of the percentage of Ascorbic acid.

3. Determination of the percentage of w/w of available chlorine.

4. Nuxvomica: Determination of the percentage of strychnine.

5. Belladonna Tincture: Determination of the percentage of w/v of alkaloids calculated as hyscyamine.

6. Soft soap: Determination of the percentage of fatty acids.

7. Conductometric Titrations.

8. Polarographic determination of Pb2+ and Zn2+.

9. Polarographic determination of heavy metals (Zn, Cd, Pb & Cu) in drinking water and natural origin

sample.

10. Recording of body temperature, pulse rate and blood pressure.


52



B.Sc.

Pharmaceutical Chemistry

Semester III

Semester III

Course Code Course Names Credits

PCH-C311 Pharmacogonosy and Phytochemistry-I 2

PCH-C-312 Pharmaceutical Biochemistry-I 2


53

PCH – C - 311

B.Sc. Pharmaceutical Chemistry -Semester III

Paper-I : Pharmacogonosy and Phytochemistry-I Credits : 2 30 Hrs

1. Pharmacognosy: Origin, scope and practice.

Metabolites: General principles of formation of primary and secondary plant metabolites 4

2. Classification of crude drugs: Alphabetical, morphological, pharmacological, chemical

and biogenetic classifications.

Biogenesis of carbohydrates: Biogenesis of carbohydrates, drugs containing

carbohydrates (starch, honey, agar, bell, lactose, pectin, ispaghula, acacia).

6

3. Volatile oils: Biogenesis of volatile oils, drugs containing volatile oil (eucalyptus,

coriander, lemon grass, mentha, cardamon, garlic, turmeric, clove, cinnamon, black-pepper,

chenopodium, caraway, turpentine oils).

4

4. Fixed oils, fats and waxes: Castor oil, cotton seed oil, neem oil, olive oil, sesame oil,

lanolin, fish liver oils, and theobroma, beeswax and spermaceti 4

5. Systematic study of crude drugs: Chemical constituents, chemical tests, uses, adulteration

and evaluation of :

(a) Alkaloids and glycosides: Classification and general treatment of alkaloids, glycosides

of different categories, biosynthesis of medicinally important glycosides and alkaloids.

(b) Glycosidal Drugs: Anthraquinone (senna, cascara, rhubarb, aloe); saponin (solanum,

senega, licorice, ginseng); cyanogenetic (wild cherry); coumarin and furano coumarin

(psoralea).

2

5

5


PCH – C - 312

B.Sc. Pharmaceutical Chemistry - Semester III

Paper-II : Pharmaceutical Biochemistry-I Credits : 2 30 Hrs

1. Foundations of Biochemistry: Cellular, chemical, physical, genetic and evolutionary foundations 3

2. Bioenergetics: Bioenergetics, phosphoryl group transfer and ATP, free energy of hydrolysis of ATP

within cells.

5

3. Water: A detailed account of water as an ideal Biologic solvent. 2

4. Enzymes: Classification, nomenclature, factors affecting enzyme action, enzyme kinetics as an

approach to understand mechanism of enzyme action, enzyme inhibition, examples of enzymatic

reactions.

5

5. Lipid Metabolism: Oxidation of fatty acids, biosynthesis of fatty acids, ketogenesis and ketosis,

biosynthesis of cholesterol, essential fatty acids, triglycerides, phospholipids metabolism.

5

6. Carbohydrate Metabolism: Classification, glycolysis, citric acid cycle, glycogenesis, hexose

monophosphate shunt, uronic acid pathway, blood sugar level and its regulation.

5

7. Bio-Redox Process: Biological oxidation-reduction reactions, oxidative phosphorylation and

photophosphorylation, enzymes and co-enzymes of bio-redox system.

5


54

PCH-C- 313

B.Sc. Pharmaceutical Chemistry - Semester III

Laboratory Course

Credits : 2

1. Determination of the primary and secondary glycosides in digitalis leaf, both calculated as

digitoxin by column chromatography.

2. Determination of Quinine in ethanolic solution by ion exchange chromatography.

3. To separate a mixture of barbiturates by TLC.

4. To separate a mixture of sulphonamides by TLC.

5. Determination of nickel with dimethylglyoxime by amperometry.

6. Determination of lead with k2Cr2O7 solution by amperometry.

7. To show the effect of solvent upon the absorption spectrum of phenol by UV-VIS

spectroscopy.

8. To show the influence of conjugated chromophores and auxochromes on chromophore by

UV-VIS spectroscopy.

9. Determination of CMC of anion (SDH / SDS) and cationic (CTAB) by conductometric /

tensio-metric methods.

10. Determination of CMC of mixed surfactants (Cationic and anionic) by conductometric /

tensio-metric methods.


55



B.Sc.


Semester IV

Semester IV


PCH-C-411 Pharmacogonosy and Phytochemistry- II 2

PCH-C-412 Pharmaceutical Biochemistry-II 2

PCH-C-413 Laboratory Exercise 2

56

PCH- C - 411

B.Sc. Pharmaceutical Chemistry - Semester IV

Paper-I - Pharmacogonosy and Phytochemistry-II

Credits : 2 30 Hrs

1. Alkaloidal Drugs: Quinoline (cinchona); Isoquinoline (opium, ipecac, curare); Quinezoline

(vasaka); Pyridine (areca, nicotiana, lobelia); Indole (rauwolfia, ergot, nux-vomica);

Imidazole (pilocarpus); Steroidal (ashwagandha, kurchi, veratrum); Terpenoid (aconite);

Protoalkaloidas (ephedra, colchicum).

8

2. Enzymes: Source, chemical nature and uses of papain, diastase, pepsin, trypsin, pancreatin,

urokinase, penicillinase, hyaluronidase.

4

3. Indigenous Traditional Drugs: Chemical constituents, pharmacological action and

clinical uses of Amla (phyllanthus emblica), Satavar (asparagus racemosus), Gokhru

(tribulu sterristris), Arjuna (terminalia arjuna), Ashok (saraca indica), Shanskpusphi

(convolvulus microphyllus), Guduchi (tinospora cordifolia), Brahmi (centella asiatica),

Tulsi (ocimum sanctum), Lahsun (allium sativum), Rasna (pluchea lanceolata)

8

4. Ayurvedic Medicine: Preparation and standardization of ayurvedic medicine such as

avaleha, aristha, asavas, churna etc.

4

5. Herbs: Detailed account of herbs as health foods and cosmetics.

Plant as agents: An overview of plants as antitumor agents, sweeterness, bitters and

photosensitizing agents

3

3


PCH – C - 412

B.Sc. Pharmaceutical Chemistry -Semester IV

Paper-II : Pharmaceutical Biochemistry-II

Credits : 2 30 Hrs

1. Amino Acids : Classification, steirochemisstry of amino acids, acid base behaviour,

isoelectric point of amino acids, end group analysis of amino acids.

6

2. Proteins Metabolism: Transamination, deamination, decarboxylation, Bioreactions of

amino acids, urea cycle, Nitrogen Balance, end products of protein metabolism, metabolism

of sulphur containing amino acids.

6

3. Nucleic Acids: Constituents of nucleic acids, isolation and structure 6

4. Metabolism of Nucleic acids: Biosynthesis and metabolism of purine and pyrimidine

nucleotides. 6

5. DNA: Biosynthesis, replication, mutation and repair mechanism.

RNA: Biosynthesis, genetic code and protein synthesis.

3

3


57

PCH-C- 413

B.Sc. Pharmaceutical Chemistry -Semester -IV

Laboratory Course

Credits : 2 30 Hrs

1. To determine the isotectic point of an indicator and to show its use in analysis.

2. Assay of Caffeine and sodium benzoate injection by the simultaneous equation.

3. Method and by the absorbance ratio by UV-VIS spectroscopy.

4. Preparation of liquid soaps and baby powders.

5. Extraction and isolation of carbohydrates, lipids, essential oils and resins.

6. Evaluation of herbal cosmetics.

7. Basic understanding of electrocardiogram PQRST waves and their significance.

8. Qualitative examination of urine, blood and faces.

9. Preparation of antiseptic cream.

10. Preparation of tooth powder of clove oil.


58




Semester V

Semester V


PCH-511 Spectroscopy-I 2

PCH-512 Medicinal and Pharmaceutical Chemistry-I 2

PCH-513 Therapeutic Agents and their Action-I 2

PCH-514 Computational Chemistry and Computer-Assisted Drug Design-I 2

PCH-515 Laboratory Course 2

Note : A modification in the scheme is under consideration.

59

PCH - 511

B.Sc. Pharmaceutical Chemistry : Semester - V

Paper-I : Spectroscopy-I

Credit(s) : 2 30 Hrs

1. Electromagnetic Radiation: General properties, characteristics of electromagnetic

radiation (emr) , types of radiation and their interaction, Photoelectric effect, Energy states,

Absorption and Emission of Radiation, Relaxation processes .

3

2. Ultraviolet–visible spectroscopy: selection Rules and intensity, Franck–Condon

principle, Born–Oppenheimer approximation, Application of Woodward-Fieser; Nielson

Rules ; Chromophores, Auxochromes, choice of solvents, Shift of bonds. Applications to

Qualitative analysis - stereoisomerism, conformational Analysis, Determination of

configurational correlation, Aromatic/Heteroaromatic/Heterocyclic Compounds, Excited

state dipole moments, Acid dissociation constant, pKa values, Kinetic studies etc.

9

3. Infrared Spectroscopy: Origin of Infrared spectra, Force constant, vibronic Transitions,

vibrations of polyatomic molecules (Linear, non linear and modes of symmetric triatomic

molecules), Number of fundamental vibrations and selection rules, Intensity and position of

Infrared bands, Factors influencing vibrational frequencies, calculation of vibrational

frequencies, Factors of simplification of infrared spectrum. Preparation of samples, choice

of solvents. Characteristic vibrational frequency of alkanes, alkenes, alkynes, aromatic

compounds, Heteroaromatic compounds, alcohols, ethers, phenols and amines. Application

of IR-spectroscopy to Qualitative analysis, conformational analysis, Isomers, Kinetic

studies etc.Basics of Fourier- Transform IR spectroscopy and its advantages.

9

4. Nuclear Magnetic Resonance: PMR: Nuclear spin, Nuclear Resonance, Equivalent and

Non-equivalent protons. Chemical Shift, Factors influencing chemical shift, chemical shift

values and correlation for protons Bo nded to carbon (aliphatic, olefinic, aldehydic and

aromatic) and other nuclei (alcohols, Phenols, enols, Carboxylic acids, amines amides and

Mercapto) Estimation of proton chemical shifts in substituted benzene. Spin-spin

interactions (systems containing two, three and three Interacting nuclei), Shielding

mechanism, Factors influencing , Nuclear Overhauser Effect (NOE).

9

Course Coordinator Prof. S.N.Limaye

60

PCH - 512

B.Sc. Pharmaceutical Chemistry : Semester - V

Paper-II : Medicinal and Pharmaceutical Chemistry-I Credits: 2 30 Hrs

1. Drug Metabolism and Action

1. Physicochemical properties: Drug distribution, acid-base properties, bonding, chelation,

charge transfer, surface activity.

2. Stereochemistry Aspects: Diastereomerism, enantiomerism, conformational isomerism,

isosterism, drug receptor interaction.

3. Pharmacokinetics: General pathways of drug metabolism, oxidative, reductive and

hydrolytic reactions, conjugative reactions, factors affecting drug metabolism, elimination.

4. Pharmacodynamics: Principles and mechanism of drug action, combined effect of drug,

factors modifying drug action.

3

3

3

3

2. Drugs Acting on Autonomic/ Somatic nervous system

1. General considerations: Organisation and function, neurohumoral transmission.

2. Cholinergic Agents: Acetyl choline-biosynthesis, storage and release, termination action.

3. Anticholinesterases: Mechanism of action, reversible inhibitors, and organophosphorous

compounds.

4. Adrenergic system and Drugs: Adrenergic transmission, sympathomimetics.

5. Local Anaesthetics: Classification, mechanism of action, adverse effects, uses and

techniques of local anaesthetics.

3

3

3

3

3

3. Autocoids

Antihistamines: Histamine life cycle, histamine H1 and H2-receptor antagonists, histamine

H3- receptor ligands,

3

Course Coordinator Prof. S. N.Limaye

61

PCH 513

B.Sc. Pharmaceutical Chemistry : Semester V

Paper-III : Therapeutic Agents and their Action


1. Drugs Acting on Central Nervous System - I

1. General Anaesthetics: Intravenous anaesthetics, mechanism of anaesthetic action.

2. Hypnotics and Sedatives: Classification, chemistry, pharmacological actions,

pharmacokinetics and adverse affects of barbiturates, benzodiazepines, BZD antagonist.

3. Opioid Analgesics: Morphine and codeine and their synthetic modifications, opioid antagonists.

4. Antiepileptics: Epilepsises, Classification, chemistry, treatment of epilepsises.

2

3

3

3

2. Drugs Acting of Central Nervous System – II

Antiparkinson’s drugs: Dopamine replacements, dopamine releasers, dopamine agonists.

Psychotropic and pharmacological Agents:

a. Antipsychotic Drugs: Psychoses, classification, mechanism of actions, adverse effects.

b. Antianxiety Drugs: Anxiety, classification, treatment of anxiety.

c. Antidepressants: MAO inhibitors, classification, mechanism of action of tricyclic and related

Antidepressants.

d. Antamanic Drugs: Mechanism, pharmacokinetics and control of therapy.

e. Hallucinogens: Introduction of indoleamines and cannabinoids.

2

2

2

2

2

3. Anticonvulsant Drugs : Barbiturates, hydantoins, oxazolidinediones, succinimides.

CNS–Stimulants: Classification and introductory ideas of different classes, cognition enhancers

4

4 Cardiovascular Agents – I

Antianginal Agents and Vasodilators: Intermediary myocardial metabolism, nitrovasodilators

metabolism and antianginal action, calcium antagonists

5

Course Coordinator

62

PCH-C-514

B.Sc. Pharmaceutical Chemistry : Semester – V

Paper-IV : Computational Chemistry and Computer-Assisted Drug Design-I


1. Introduction to QSAR

Historical development, site specific (drug receptor interaction) and need for QSAR, role of

physicochemical parameters in chemical structure and biological activity;

Physicochemical parameters viz., lipophilicity, polarizability, electronic and steric

parameters involved in qualitative and quantitative relationship in biological and chemical

structure, Lipophilicity : partition coefficients and chromatographic parameters;

Polarizability – molecular refractivity, molar volume, parachore etc., electronic – Hammete

constant, field and resonance, charge transfer, steric parameters : conformational and

geometric considerations

4

6

2. Molecular Force Fields

Molecular force fields: definition and their types and mathematical relationships, Eminimization

significance of molecular force fields;

Toplogical parameters:

Toplogical parameters: definition, notations and molecular graph, connectivity indices and

types of topological parameters – Winner, Balaban, etc,

4

4

3. QSAR Models

QSAR Models, LFER- linear free energy relationship, Free Wilson Method of Additive

Model; Hansch’s method of Extra Thermodynamic Approach; Kubinyi Mixed approach of

non linear relationship.

8

4 Application of QSAR:

Isolated receptor interactions, interaction at cellular level, interaction in vivo.

4

Course Coordinator

PCH - 515

B.Sc. Pharmaceutical Chemistry, Semester - V

Laboratory Exercise

Credit(s) : 2

Synthesis of aspirin and its electrometric or chemical analysis.

Electrometric or chemical analysis of Metranidazole.

Preparation and evaluation of cold cream, vanishing cream, after-shave lotions,

Shampoo, sunscreen, dental care, mouthwashes, hair colorants etc.

Estimation of glucose, creatinine, proteins and amino acids in body fluids.

Determination of Cholesterol, cretinines.

Preparation and purification of some simple inorganic compounds of pharmaceutical importance alumina

gel, magnesia gel

Course Coordinator

63




Semester VI

Course Code

Course Name Credits

PCH-611 Spectroscopy-II 2

PCH-612 Medicinal and Pharmaceutical Chemistry-II 2

PCH-613 Therapeutic Agents and their Action-II 2

PCH-614 Computational Chemistry and Computer-Assisted Drug Design-II 2

PCH-615 Laboratory Course 2

Note : A modification in the scheme is under consideration.

64

PCH-C- 611

B.Sc. Pharmaceutical Chemistry : Semester - VI

Paper-I : Spectroscopy-II

Credits : 2 30 Hrs

1. 13C NMR: General considerations, chemical shift of carbon nuclei (aliphatic, olefinic, aromatic,

heterocyclic and carbonyl carbon), coupling constants, off Resonance Decoupling. Estimation of 13

C–

chemical shifts (aliphatic chains, substituted alkenes and substituted Benzene). Other Nuclei:

Application of NMR to phosphorous – 31 and fluorine – 19 Nuclei. Applications of NMR in clinical /

diagnostic purposes.

8

2. Mass Spectrometry: Introduction, Ion production (Electron Impact, chemical Ionisation, Field

Ionisation, Fast Atom Bombardment, Secondary ionization mass spectroscopy. Factors affecting

fragmentation, ion analysis , Ion abundance, Basics of separation of ions, Fragmentation of organic

compounds of classes of common functional groups, Molecular Ion peak, Isotope peaks, metastable

peaks, Nitrogen rule, Ring rule, Index Hydrogen Deficiency. Molecular weight determination,

Determination of molecular formula,

8

3. Application of Mass spectrometry: to Trace levels of pharmaceuticals and Disinfections, Byproducts

in water supplies; Methyl esters of fatty acids; Drugs of Abuse; malaria Detection and Diagnosis.

Bioanalytical mass spectrometry to proteomics

8

4 Combinatorial spectroscopy: Joint application of UV-VIS, IR, H1 and

13C–NMR and mass spectral

data for structure elucidation of some compounds.

6

Course Coordinator Prof. S. N. Limaye

PCH-C- 612

B.Sc. Pharmaceutical Chemistry; Semester – VI

Paper-II : Medicinal and Pharmaceutical Chemistry-II

Credits : 2 30 Hrs

1. Autocoids

Eicosanoids: Chemistry, biosynthesis and degradation of prostaglandins and leukotrienes, drug

action mediated by eicosanoids, eicosanoid receptors. Concept of NSADS (Nonopioid Analgesics and

Nonsteroidal Antiinflammatory Drugs),

8

2. Harmones and Related Drugs

Thyroid Harmones: Chemistry and synthesis, transport, metabolism and excretion, actions.Thyroid

inhibitors: Classification, antithyroid drugs, β adrenergic blockers.

Insulin and oral Hypoglycaemic agents: Insulin, assay, regulation of insulin secretion, actions, insulin

preparations, oral hypoglycaemic drugs (sulfonyl ureas, status in diabetes mellitus), glucagons.

Drugs affecting calcium Balance: Physiological roles, absorption and excretion of calcium, actions

and uses of parathormone, calcitonin and vitamin D.

8

3. Diuretics/gastrointestinal Drugs

Diureties: Anatomy and physiology of nephron, functions of nephrons, Carbonic Anhydrase

inhibitors, Thiazide, thiazide like diuretics and their mechanism of action, High-ceiling or Loop

Diuretics.

8

4 Gastrointestinal Drugs: peptic ulcer, Regulation of gastric acid secretion, Antagonists,

pharmacological actions, ulcer protectives. Introductory idea of Emetics, Antiemetics

6


65

PCH –C-613


Paper-III : Therapeutic Agents and their Action-II

Credits : 2 30 Hrs

1. Cardiovascular Agents – I

Antiarrhythmic Drugs: Cardiac electrophysiology, mechanism of Arrhythmias,

Classification, pH and activity of Antiarrhythmic drugs.

Antihypersensive agents: Renin–Angiotensin system and hypertension,

Renin–Angiotensin system inhibitors, Adrenergic system inhibitors, potassium channel

Agonists.

10

2. Cardiovascular Agents – II

Antihyperlipidemic Agents: Lipoprotein classes, metabolism, Hyperlipoproteinemias, HMG-

Co A Reductase Inhibitors

Anticoagulants and Antiplatelet Drugs: Mechanism of blood coagulation, anticoagulant

mechanism, oral anticoagulants, platelet aggregation and Inhibitors.

Cardiac Glycosides: Chemistry, pharmacological Actions, mechanism of action, congestive

Heart failure

10

3. Chemotherapeutic Agents:

Antimalarials: Malaria, malarial vaccines, Drug therapy (Cinchona Alkaloids), New

Antimalarial drugs.

Antitubercular Drugs: Tuberculosis, Antitubercular drugs (Isoniazid, Rifampm ,

pyrzinamide,Ethambutol (E), Newer drugs, Treatment of Tuberculosis

10


66

PCH-C- 614


Paper-IV : Computational Chemistry and Computer-Assisted Drug Design-II

Credits : 2 30 Hrs

1. Minimisation :

Molecular force fields in minimization and conformational search; Process of minimization, global

and local minimization, minimization algorithm – derivative and non derivatives methods- steepest

descent, newton Raphson, Conjugate gradiants, variable mattrics, suitable examples;

Conformational Search and Molecular Dynamics :

Systematic and semi-random search (Monte Carlo) , genetic algorithm and distance geometry,

process of modeling, parameters of molecular dynamics, dynamic simulation, simulation annealing,

free energy calculation, analysis of results and applications,

5

5

2. Statistical Methods in QSAR :

Regression, significance, partial least square, mono-, di- and multi variate correlation, Craig’s plots,

Topliss method, Physicochemical parameters and biological activity : Mayor-Overton Theory,

Fergusion theory, Taft’s plots, Verloop, Steric parameters.

Application of Hansch’s approach, pharmaco- kinetic data, biological data, activity-activity

relationship, Application of Free Wilson relationship,

7

3

3. Stereochemistry and drug action.

Active site interaction, comparative molecular field analysis (CoMFA), molecular similarity analysis,

factors governing drug ability to reach active site – adsorption, distribution, metabolism, excretion,

Known / Unknown receptors: Definition and characterization of site, Design of ligand :

Pharmacophore versus binding site models, searching for similarity, molecular comparisons,

common pattern findings.

Stereochemistry of drug designing, Introductory idea of ADME and some other available softwares,

screening libraries for Lead identification pharmacophore screening.

5

5


PCH-C- 615

B.Sc. Pharmaceutical Chemistry, Semester - VI

Laboratory Course

Credits: 2

To determine the percentage of menthol in peppermint oil by GLC.

2. To determine the composition of the fatty acid by GLC.

3. Separation and identification of the xanthenes derivatives in tea or coffee by HPLC.

4. Separation of penicillin and the quantitative assay of ampicillin and cloxacillin in

a powder for injection by HPLC.

5. Determination of calcium in magnesium chloride for dialysis by AES.

6. Determination of total zinc in insulin zinc suspension by AAS.

7. The assay of Ca and Mg in serum by AAS.

8. Determination of the amount of phenobarbitone in phenobarbitone tablets by IR.

9. To determine the percentage of menthol in peppermint oil by IR method.

10. Assay of meprobamate in meprobamate tablets by UV& Vs.

11. Identification by joint application of UV-VIS, IR, 1H,

13C and mass spectroscopic methods.

12. Estimation of Na+, K

+, Ca

2+ ions by flame photometry.


67



B.Sc.


Semeter V

Proposed 2014-15


PCH-C-511 Medicinal and Pharmaceutical Chemistry 2

PCH-C-512 Computational Chemistry –I 2


Note : Under consideration

68

PCH - 511

B.Sc. Pharmaceutical Chemistry -Semester V

Paper-I : Medicinal and Pharmaceutical Chemistry

02 Credits 30 Hrs 1. Drug Metabolism and Action : Pharmacokinetics: General pathways of drug metabolism,

oxidative, reductive and hydrolytic reactions, conjugative reactions, factors affecting drug

metabolism, elimination. Pharmacodynamics: Principles and mechanism of drug action,

combined effect of drug, factors modifying drug action.

10

2. Autocoids : Introductory idea about Histamines : Histamine life cycle, histamine H1 and H2-

receptor antagonists, histamine H3- receptor ligands.

Eicosanoids: Chemistry, biosynthesis and degradation of leukotrienes, drug action mediated

by eicosanoids, eicosanoid receptors.

4

3. Harmones and Related Drugs : Thyroid Harmones: Chemistry and synthesis, transport,

metabolism and excretion, actions.Insulin and oral Hypoglycaemic agents: Insulin, assay,

regulation of insulin secretion, actions, oral hypoglycaemics drugs (sulfonyl ureas, status in

diabetes mellitus), glucagons.Drugs affecting calcium Balance: absorption and excretion of

calcium, actions and uses of parathormone, calcitonin and vitamin D.

8

4. Diuretics/gastrointestinal Drugs : Diureties:Structure ,Synthesis,Pharmacological properties

,Adverse effect of Carbonic Anhydrase inhibitors, Thiazide, thiazide like diuretics and their

mechanism of action, High-ceiling or Loop Diuretics.

Introductory idea about Gastrointestinal Drugs: peptic ulcer secretion, Introductory idea of

Emetics, Antiemetics

8

Course Coordinator Dr. Poonam Kohli

PCH-C-512

B.Sc. Pharmaceutical Chemistry : Semester – V

Paper-IV : Computational Chemistry and Computer-Assisted Drug Design-I

Credits : 2 30 Hrs

1. Introduction to QSAR

Historical development, site specific (drug receptor interaction) and need for QSAR, role of

physicochemical parameters in chemical structure and biological activity;

Physicochemical parameters viz., lipophilicity, polarizability, electronic and steric parameters involved

in qualitative and quantitative relationship in biological and chemical structure, Lipophilicity : partition

coefficients and chromatographic parameters; Polarizability – molecular refractivity, molar volume,

parachore etc., electronic – Hammete constant, field and resonance, charge transfer, steric

parameters : conformational and geometric considerations

4

6

2. Molecular Force Fields : Molecular force fields: definition and their types and mathematical

relationships, Eminimization significance of molecular force fields;

Toplogical parameters: Toplogical parameters: definition, notations and molecular graph, connectivity

indices and types of topological parameters – Winner, Balaban, etc,

4

4

3. QSAR Models: QSAR Models, LFER- linear free energy relationship, Free Wilson Method of Additive

Model; Hansch’s method of Extra Thermodynamic Approach; Kubinyi Mixed approach of non linear

relationship.

8

4 Application of QSAR: Isolated receptor interactions, interaction at cellular level, interaction in vivo. 4


69

PCH -C- 513


Semester – V

Laboratory Course

Credits : 02 30 Hrs

1. Synthesis of aspirin and its electrometric or chemical analysis.

2. Electrometric or chemical analysis of Metranidazole.

3. Preparation and evaluation of cold cream, vanishing cream, after-shave lotions,

4. Shampoo, sunscreen, dental care, mouthwashes, hair colorants etc.

5. Estimation of glucose, creatinine, proteins and amino acids in body fluids.

6. Determination of Cholesterol, cretinines.

7. Preparation and purification of some simple inorganic compounds of pharmaceutical

importance alumina gel, magnesia gel

8. To determine the percentage of menthol in peppermint oil by GLC.

9. To determine the composition of the fatty acid by GLC.

10. Separation and identification of the xanthenes derivatives in tea or coffee by HPLC.

11. Separation of penicillin and the quantitative assay of ampicillin and cloxacillin in a powder for

injection by HPLC.

12. Determination of calcium in magnesium chloride for dialysis by AES.

13. Determination of total zinc in insulin zinc suspension by AAS.

14. The assay of Ca and Mg in serum by AAS.

15. Determination of the amount of phenobarbitone in phenobarbitone tablets by IR.

16. To determine the percentage of menthol in peppermint oil by IR method.

17. Assay of meprobamate in meprobamate tablets by UV& Vs.

18. Identification by joint application UV-VIS, IR, 1H,

13C and mass spectroscopy method.

19. Estimation of Na+, K

+, Ca

2+ ions by flame photometry

Course Coordinator Dr. Poonam Kohli

.

70



B.Sc.


Semeter VI

Proposed 2014-15


PCH-C-611 Therapeutic Drugs and Agents 2

PCH-C-612 Computational Chemistry –II 2

PCH-C-613 Laboratory Course-Project work on QSAR 2

Note Under Consideration

71

PCH 611

B.Sc. Pharmaceutical Chemistry- Semester V

Paper-I : Therapeutic Drugs and Agents

Credits : 2 30 Hrs

1. Drugs Acting on Central Nervous System – I General Anaesthetics: mechanism of anaesthetic action

- Hypnotics and Sedatives: Classification, chemistry, pharmacological actions, pharmacokinetics and

adverse affects of barbiturates, benzodiazepines, BZD antagonist.

6

2. Drugs Acting of Central Nervous System –II General introduction and idea about Antiparkinson’s

drugs: Dopamine replacements, dopamine releasers, dopamine agonists: Classification, action and

adverse effect of a.Antipsychotic b. Antianxiety c. Antidepressants: d. Antamanic Drugs: e.

Hallucinogens,f. CNS–Stimulants.

8

3. Cardiovascular Agents : Anti-anginal Agents and Vasodilators: Intermediary myocardial metabolism,

nitro-vasodilators metabolism, Anti-arrhythmic Drugs. Anti-hypersensive agents:

General introductory idea about Cardiac Glycosides: Chemistry, pharmacological Actions,

mechanism of action, congestive Heart failure.

8

4. Chemotherapeutic Agents: Antimalarials: Malaria, malarial vaccines, Drug therapy (Cinchona

Alkaloids), New Antimalarial drugs. Antitubercular Drugs: Tuberculosis, Antitubercular drugs

(Isoniazid, Rifampm, pyrzinamide,Ethambutol (E), Newer drugs, Treatment of Tuberculosis.

8


PCH-C- 612


Paper-IV : Computational Chemistry and Computer-Assisted Drug Design-II

Credits : 2 30 Hrs

1. Minimisation : Molecular force fields in minimization and conformational search; Process of

minimization, global and local minimization, minimization algorithm – derivative and non derivatives

methods- steepest descent, newton Raphson, Conjugate gradiants, variable mattrics, suitable

examples;

Conformational Search and Molecular Dynamics :Systematic and semi-random search (Monte

Carlo) , genetic algorithm and distance geometry, process of modeling, parameters of molecular

dynamics, dynamic simulation, simulation annealing, free energy calculation, analysis of results and

applications,

5

5

2. Statistical Methods in QSAR : Regression, significance, partial least square, mono-, di- and multi

variate correlation, Craig’s plots, Topliss method, Physicochemical parameters and biological activity

: Mayor-Overton Theory, Fergusion theory, Taft’s plots, Verloop, Steric parameters.Application of

Hansch’s approach, pharmaco- kinetic data, biological data, activity-activity relationship, Application

of Free Wilson relationship,

7

3 3. Stereochemistry and drug action.

Active site interaction, comparative molecular field analysis (CoMFA), molecular similarity analysis,

factors governing drug ability to reach active site – adsorption, distribution, metabolism, excretion,

Known / Unknown receptors: Definition and characterization of site, Design of ligand :

Pharmacophore versus binding site models, searching for similarity, molecular comparisons,

common pattern findings.

Stereochemistry of drug designing, Introductory idea of ADME and some other available softwares,

screening libraries for Lead identification pharmacophore screening.

5

5


72

PCH 613


Semester - VI

Laboratory Course : Project work on QSAR

Credits: 02

1. Exercises related with computational work on known drugs, their biological activities and

structural correlations : Examples : Barbiturates, Phenyl derivatives , isoxazole and

isoxazoline drugs.

department of chemistry dr. harisingh gour vishwavidyalaya ... - pch... · dr. harisingh gour...

Documents