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PHAR. CHEMISTRY -VI PY-503 SYLLABUS
Introduction to medicinal chemistry 
  • Principles of drug discovery: Basic principles of medicinal chemistry,physicochemical and steric aspects (optical, geometric and bioisosterism) of drug molecules and biological actions.
  • Receptors and drug action: Receptor theories, affinity, receptor and biologic response.
  • Drug metabolism: Phase I (biotransformation reactions), phase II (conjugation reactions), factor affecting drug metabolism.
  • Prodrugs and drug latentiation: Basic concepts, prodrug of functional groups, bioprecursor prodrugs, chemical delivery system. Classification and mode of action, uses, structure activity relationship including physicochemical, steric aspects and resents advances in research of the following categories of drugs:
  • Drugs affecting neurotransmission
  • Drugs affecting cholinergic neuro transmission: Neuro chemistry and stereochemistry of acetylcholine, acetylcholine mimetics-muscarinic agonists,acetlycholinesterase inhibitors, acetylcholine antagonists-muscarinic anatagonists, nicotinc antagonists-neuromuscular blocking agents, ganglionic blocking agents.
  • Drugs affecting adrenergic neurotransmission: Neurochemistry and stereochemistry of norepinephrine, sympathomimetic agents, sympatholytic agents, drugs affecting catecholamine biosynthesis, drugs affecting catecholamine storage and release, ergot alkaloids, xanthine bronchodilators
  • Drugs affecting serotonergic neurotransmission: Neurochemistry and stereochemistry of serotonin, 5-HT agonists, 5-HT antagonists.
  • Local anesthetics: Molecular mechanism of action, chemical aspects.
  • Drugs affecting immune systems
  • Non-steroidal anti-inflammatory agents: Chemistry of chemical mediators of inflammation (prostaglandins, thromboxanes, prostacyclin and leukotrienes), antipyretic analgesics.
  • Antihistaminics and related antiallergics: Neurochemistry and stereochemistry of histamine, inhibitor of histamine release (mast cell stabilizers), inhibitors of released histamine, dual acting antihistaminics; H2 antagonists, H3 antagonists.
LIST OF PRACTICALS:
(Minimum fifteen experiments should be performed in the semester. Student should aware with safety parameters and handling of chemicals related to following experiments)
  • Synthesis and characteriazation of Tropenone from Maleyde aldehyde.
  • Synthesis and characteriazation of Scopolamine from Tropenol.
  • Synthesis and characterization of chlorzoxazone from 2-amino-4-chlorphenol.
  • Synthesis and characterization of Clemastine.
  • Synthesis and characterization of Tripelennamine.
  • Synthesis and characterization of Oxyphenbutazone.
  • Synthesis and characterization of trihexyl phenylidine.
  • Synthesis and characterization of Aspirin from salicylic acid.
  • Synthesis and characterization of Benzimadazole from benzyl chloride.
  • Synthesis and characterization of Sulphonilamide from Aniline.
  • Synthesis and characterization of Paracetamol from Para amino phenol.
  • Synthesis and characterization of Ibuprofen from isobutyl benzene.
  • Synthesis and characterization of Antipyrine
  • Synthesis and characterization of Phenyl benzoate.
  • Synthesis and characterization of Benzenilide.
  • Synthesis and characterization of Phenindione.
  • Synthesis and characterization of Methyl pyrazolone.
BOOKS RECOMMENDED: 
  • Foye, W.C., Principles of Medicinal Chemistry, Lea and Febiger, Philadelphia.
  • Wolff , M.E. Ed., Burger’s Medicinal Chemistry, John Wiley and Sons, New York.
  • Hansch, C., Comprehensive Medicinal Chemistry, Pergarnon Press, Oxford.
  • Delagado, J.N. and Remers, W.A.R, Wilson and Giswold’s Text Book of Organic,Medicinal and Pharmaceutical Chemistry, J.Lippincott Co., Philadelphia.
  • Nogrady, T., Medicinal Chemistry-A Biochemical Approach, Oxford University Press, New York, Oxford.
  • Kar, A., Medicinal Chemistry, Willey Eastern Ltd., New Delhi.
  • Patrick, G., An Introduction to Medicinal Chemistry, Scientific Distributors, Mumbai.
  • Malone, Dyson and Purey, May’s Chemistry of Synthetic Drugs.
  • Parimoo, P., Text Book of Medicinal Chemistry, CBS Publishers and Distributors, New Delhi.
  • Thomas, G., Introduction to Medicinal Chemistry, CBS Publishers and Distributors, New Delhi 
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PHARMACEUTICAL CHEMISTRY-III PY-203 (ORGANIC-I) SYLLABUS
UNIT-I
Structure and Properties:Electronegativity,Polarity, Resonance;Electrophiles/Nucleophiles, Orbitals, π-Bonds, Hybridization and Shape, Isomerism, Polarity, Intermolecular Forces, isotope effects and isotopic labelling.

UNIT-II

Reactive Intermediates: Stability and reactivity of Radicals, Cations, Anions, Nitrene and Nitrenium ion

UNIT-III
Stereochemistry:Stereo-isomerism, classification and Nomenclature,Optical activity, Chirality, R/S Classification of Chiral Carbons. Miscellaneous Stereochemistry, Diastereomers; Racimic modification, Resolution of racimic mixtures.

UNIT IV

Hydrocarbons: Alkanes and cycloalkanes:Nomenclature, Physical and chemical properties of alkanes, Conformations and Stability of Acyclic Alkanes and Cycloalkanes.  
Alkenes and alkynes:Nomenclature,Physical and Chemical properties of alkenes, isomerism, and general methods of preparation. 
Aromatic hydrocarbons:Benzene and its homologues (Polynuclear compounds), nomenclature,sources of aromatic hydrocarbons, structure of benzene, chemical reaction of benzyne-mechanism and SNAr Mechanism of nucleophilic substitution. Directive influence of substituents and their effect on reactivity. 
Dienes and the Allyl system: Conjugation, Reactivity.

UNIT-V
Organic compounds with functional groups containing halogens (X): Nomenclature, Structure, Properties, Reactivity of Alkyl Halides (haloalkanes and haloarenes): The SN2 and SN1 Substitution Reaction, The E1 and E2 Elimination Reactions, Substitution vs. Elimination reaction, reactivity of C-X bond in haloalkanes and haloarenes

UNIT VI

Organic compounds with functional groups containing oxygen (Part I-): Alcohols: Nomenclature, Synthesis, reactivity of different Alcohols; conversion of Alcohols to Tosylates or Halides.
Phenols: Nomenclature, methods of preparation, physical and chemical properties; chemical reactivity of phenols in electrophilic substitutions, acidic nature of phenol. 
Ethers: electronic structure, structure of functional group, nomenclature,important methods of preparation, physical and chemical properties, some commercially important compounds.

UNIT-VII
Organic compounds with functional groups containing oxygen (Part II): Aldehydes and ketones : Electronic structure of carbonyl group, nomenclature, important methods of preparation, physical properties and chemical reactions, relative reactivity of aldehydic and ketonic groups, aldol condensation. nucleophilic addition reaction to >C=O groups.
Carboxylic acids: Electronic structure of -COOH, Nomenclature, important methods of preparation, physical properties and effect of substituents on α-carbon on acid strength, chemical reactions. 

Derivatives of carboxylic acids: Electronic structure of acid chloride, acid anhydride, ester and amide groups, Nomenclature, important methods of preparation, comparative reactivity of acid derivatives.

UNIT-VIII

Organic Compounds with functional group containing Nitrogen: Structure, Nomenclature of Amino and Diazo Compounds. 
Amines: Primary, secondary and tertiary amines, a general awareness, important methods of preparation, physical properties, basic character of amines, chemical reactions. 
Diazonium salts:Preparation, chemical reaction and uses of Benzene diazonium chloride. Some commercially important nitrogen containing carbon compounds(Aniline, TNT)

LIST OF PRACTICALS:

  • Purify the given organic compounds by distillation.
  • Purify the given organic compounds by recrystillazation.
  • Introduction to the use of stereo models.
  • Synthesis, Purification, Characterization (by using Solubility, Melting Point,T.L.C. and percentage purity) of organic compounds and percent yield calculations of the following compounds:
  • a) 2, 4, 6-trinitro phenol (Picric acid) from phenol
  • b) Iodoform from ethyl alcohol
  • c) 2, 4, 6-tribromoaniline from aniline
  • d) 2, 4, 6-tribromo phenol from phenol
  • e) Phenylbutazone from phenol
  • f) Benzanilide from aniline
  • g) Phthalidimide from phthalic anhydride
  • h) Thiourea
  • i) Phenyl urea
  • j) Flourescein
  • k) Methly orange
  • l) Methly red
BOOKS RECOMMENDED:
  • Organic Chemistry, R.T. Morrison and R.N. Boyd, 6th Edition, New York.
  • Organic Chemistry, T.W.G. Solomons, 8th Edition, John Wiley & Sons, Inc
  • Advanced Organic Chemistry, J. March, Reaction Mechanisms and Structure, John Wiley and Sons, N.Y.
  • Mechanisms and structure in Organic Chemistry, E.S. Gould, Hold Rinchart and Winston, New York.
  • Advanced Organic Chemistry, Reaction Mechanisms, Bernard Miller, 2nd edition, Pearson education Ptc. Ltd. Singapore.
  • Named Organic Reactions, Thomas Lane & Andreas Plagens, 2nd edition, John Wiley and Sons, N.Y).
  • Organic Chemistry Finar Vol-1 & 2.
  • Structure and Mechanism in Organic Chemistry, Ingold, C. K., Cornell University.
  • Stereochemistry of Carbon Compounds, Eliel, E.L., McGraw Hill, New York.
  • Elements of Stereochemistry, Eliel, E.L., Wiley, New York.

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