NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester III) Class : M. Sc final year Section: Organic Chemistry Course/Paper: I- CH(OC) 301T: Organic Chemistry, Unit: Synthetic reagents I No. of Hours Allotted: 15 Topics to be covered No. of Hours required Introduction to reactions and reagents 1 i) Protecting groups: a) Protection of alcohols by ether, silyl ether and ester formation 1 b) Protection of 1,2-diols by acetal, ketal and carbonate formation 1 c) Protection of amines by benzyloxycarbonyl, t-butyloxycarbonyl, fmoc and triphenyl methyl groups. 1 d) Protection of carbonyls by acetal, ketal and thiolacetal (Umpolung) groups 1 e) Protection of carboxylic acidsS by ester and ortho ester (OBO) formation. 1 ii)Organometallic Reagents: Preparation and application of the following in organic synthesis: 1) Organo lithium 1 2) Organo copper reagents 3) Organo boranes in C-C bond formation 1 4) Organo silicon reagents: reactions involving β-carbocations and αcarbanions, utility of trimethyl silyl halides, cyanides and triflates 1 iii)Carbonyl methylenation: a) Phosphorous ylide mediated olefination 1) Witting reaction, 1 2) Horner-Wordsworth-Emmons reaction.b) Titanium- Carbene mediated olefination 1) Tebbe reagent, 1 2) Petasis reagent 3) Nysted reagent iv) Carbene insertions: Rh based carbene complexes, cyclopropanations. 1 v) C-H Activation: Introduction, Rh catalysed C-H activation. 1 Over view of the topic 1 Seminar by students 1 15hrs Name of the Teacher: Dr.B.Sakram Head, Department of chemistry Signature: Signature:
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NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester III)
Class : M. Sc final year Section: Organic Chemistry
Course/Paper: I- CH(OC) 301T: Organic Chemistry,
Unit: Synthetic reagents I No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Introduction to reactions and reagents 1
i) Protecting groups: a) Protection of alcohols by ether, silyl ether and ester formation
1
b) Protection of 1,2-diols by acetal, ketal and carbonate formation
1
c) Protection of amines by benzyloxycarbonyl, t-butyloxycarbonyl, fmoc and triphenyl methyl groups.
1
d) Protection of carbonyls by acetal, ketal and thiolacetal (Umpolung) groups 1
e) Protection of carboxylic acidsS by ester and ortho ester (OBO) formation.
1
ii)Organometallic Reagents: Preparation and application of the following in organic synthesis: 1) Organo lithium
1
2) Organo copper reagents 3) Organo boranes in C-C bond formation 1
4) Organo silicon reagents: reactions involving β-carbocations and αcarbanions, utility of trimethyl silyl halides, cyanides and triflates
1
iii)Carbonyl methylenation: a) Phosphorous ylide mediated olefination 1) Witting reaction,
Unit: OC (CB3) -10: Green Synthesis No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
i) Microwave Assisted Organic Synthesis (MAOS): introduction, benefits and limitations
1
a) Microwave assisted reactions in organic solvents: Esterification, Fries rearrangement
1
a) Microwave assisted reactions in organic solvents: Claisen rearrangement and Diels- Alder reaction
1
b)Microwave assisted Solvent-free reactions: Deacetylation, saponification of esters, alkylation of reactive methylene compounds and synthesis of nitriles from aldehydes.
1
ii)Ultrasound Assisted Organic Synthesis: introduction, applications of ultrasoundCannizaro reaction,
1
ii)Ultrasound Assisted Organic Synthesis: introduction, Reformatsky reaction and Strecker synthesis
1
iii)Organic Synthesis in Green Solvents: introduction a) Aqueous Phase Reactions: Diels-Alder Reaction, Heck reaction,
1
Hoffmann elimination, Claisen-Schmidt condensation hydrolysis and dihydroxylationreactions.
1
b)Organic Synthesis using Ionic liquids: Introduction, applications-Beckmann rearrangement
1
Organic Synthesis using Ionic liquids: Introduction, Suzuki Cross-Coupling Reaction and Diels- Alder reaction.
1
iv) Green Catalysts in organic synthesis: introduction a) Phase Transfer Catalysts in Organic Synthesis: Introduction, Williamson ether
synthesis and Wittig reaction
1
Biocatalysts in Organic Synthesis: Biochemical (microbial) oxidations 1
Biocatalysts in Organic Synthesis: Reductions. 1
Over view of the topic 1
Seminar by students 1
15hrs
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018
Class : M. Sc final year Section: Organic Chemistry
Solid phase synthesis, types of resins. Linkers. 1
Reactants for solid phased synthesis. 1
Methods of Parallel synthesis: Haughton’s tea bag procedure. 1
Automated parallel synthesis 1
Methods in Mixed combinatorial synthesis: general principles. 1
Furkas mix and split combinatorial synthesis, 1
Structure determination of active compounds-Deconvolution, 1
Methods in deconvolutionrecursive deconvolution, tagging and use of decoded sheets 1
. Examples of Combinatorial Chemistry. 1
Planning and designing of combinatorial synthesis 1
Spider like scaffolds, drug molecules. 1
Automation in Combinatorial chemistry 1
High throughput screening. 1
15hrs
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Course/Paper: II- CH(OC) 21: Organic Chemistry,
Unit: Drugs acting on metabolic process,cell wall,and specific enzymes
No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Classification of drugs, Chemotherapeutic agents and Pharmacodynamic agents. Introduction to macromolecular targets.
1
Classification of targets of drug targets – Drugs acting on metabolic process, cell wall and specific enzymes , Drugs acting on genetic material DNA /RNA and immune system ,Drugs acting on receptors and ion channels
1
:Drugs acting on Antifolates; Identification ,Sulphonamides . activity in in-vivo and in-vitro .
1
Synthesis of sulfomethoxazole, sulfodoxine, sulfaguanidine and dapsone. Diaminopyrimidines –trimethoprim.
1
Folate Metabolism – Sites of inhibition by Sulphonamides and Diaminopyrimidines –trimethoprim.
1
Drug Synergism . Sulphones –Anti leprotic – synthesis. 1
:Bacterial cell wall structure ( Gram-ve &gram +ve) . biosynthesis of Pencillins and cephalosporins. Synthesis of pencillin-G and cephalosporin-C
1
Mechanism of action of β-Lactam antibiotics to inhibit transpeptidation. 1
Resistance to pencillins, identification of broad spectrum penicillins – cloxacillin, methicillin, ampicillin, amoxicillin and carbenicillin.
1
Resistance to cephalosporins. identification of broad spectrum cephalosporins. Cephalothin , cephadroxyl.cephalochlor &cephalexin Synthesis of cephalexin and cycloserine
1
. Bacterial resistance, β-Lactamase inhibitors- Structuress and mode of action of clavulanic acid , sulbactum and YTR-830
1
Drugs acting on enzymes- Introduction of H2 and H1 receptors. 1
Asymmetric aldol reaction: Diastereoselective aldol reaction (achiral enolate & achiral aldehydes ) its explanation by Zimmerman-Traxel model.
1
Carbonic anhydrase inhibitors- Diuresis , Equilibrium of H2CO3, Synthesis and mode of action of Acetazolamide
15hrs
Name of the Teacher:Dr.P.Saritha Rajender Head, Department of chemistry
Signature: Signature:
OC-22: Drugs acting on genetic material and immune system
1. Drugs acting on genetic material: Introduction, classification and mechanism of
action.
2. DNA-intercalating agents: Anticancer and antimalarial agents. Structural formulae of
Daunomycin, Adriamycin and Amsacrine
3. Synthesis of Amscarine, Nitracrine, Quinacrine and Chloroquine.
4. DNA- Binding and nicking agents: : Antiprotozoal drugs
5. Synthesis of Metronidazole, Dimetridazole and Tinidazole.
6. DNA-Alkylators: Synthesis of Cyclophosphamide and Bisulphan
7. DNA-Polymerase inhibitors: Antiviral agents- Synthesis of Acyclovir and AZT.
8. DNA-Topoisomerase inhibitors: Anti bacterial agents.Synthesis of Ciprofloxacin and
Norfloxacin.
9. Structural formulae ofloxacin and Lomefloxacin.
10. Inhibitors of transcribing enzymes: Anti-TB and antileprosy agents-structural
formulae of Rifamycins and partial synthesis of Rifampicin.
11. Drugs interfering with translation process: Antibacterial drugs- Structural formulae of
Erythromycin, 5-Oxytetracycline and Streptomycin.
12. Synthesis of Chloromycetin Drugs acting on immune system: Introduction to immune
system.
13. Immunosupressing agentstructural formula of Cyclosporin.
14. Immunoenhancers-use of vaccines
15. strucrural formula of levamisol.
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Course/Paper: II- CH(OC) 21: Organic Chemistry,
Unit: OC-23: Drugs acting on receptors and ion channels
No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Introduction to nervous system: structure of neuron, nerve transmission. 1
Definition and examples of agonist, antagonist, neurotransmitters and receptors 1
Drugs acting on receptors:Adrenergic receptors - Introduction and classification. 1
α-Adrenergic-receptor agonists and antagonists 1
Synthesis and biological activity of Nor-adrenaline, Methyl L dopa and Tetrazosin. 1
β-Adrenergic-receptor - agonists and antagonists – Synthesis and pharmacological activity of Salbutamol, Tetrabutalin, Propranolol and Atenolol
1
Cholinergic-receptors: Introduction and classification. Cholinergic-receptor agonists and antagonists-
1
Structural formulae of Nicotine, Atropine and Tubocurarine. Synthesis of Acetyl choline and Succinyl choline
1
Dopamine receptors: Introduction and classification. Dopamine- receptor agonists and antagonists- Biosynthesis of Dopamine. Synthesis of L-Dopa and Chlorpromazine.
1
Serotonin receptors: Introduction and classification. Serotonin receptor agonists and antagonists-synthesis and pharmacological activity of Serotonin and Metoclopramide
1
)Histamine receptors: Introduction and classification. Histamine receptor agonists and antagonists-
1
synthesis and biological action of Histamine, Chloropheneramine, and Ranitidine. 1
Hormones and their receptors: Introduction to estrogen receptors, Structural formulae of Tamoxifen
1
Drugs acting on ion channels: Introduction to ion channels, drugs acting on Ca2+, Na+ and Cl- channels and their mode of action
1
Structural formulae of Tetracaine and synthesis and of Nifedipine, Diltiazem, Tetracine and 4-Aminopyridine
1
15hrs
OC-32:Chiraldrugs 15hrs
1. Introduction to chiral drugs. Three-point contact model.
2. Eutomer, Distomer and eudesmic ratio. Pfeiffer’s rule.
3. Role of chirality on biological activity: Distomers – a) with no side effects
4. b)with undesirable side effects c) both isomers having independent therapeutic value
5. d)combination products having therapeutic advantages.
6. e) metabolic chirality inversion.
7. Synthesis and pharmacological activity of S-Ibuprofen, S- Metaprolol.
8. Synthesis and pharmacological activity of Ininavir sulfate, Levocetrazine.
9. Synthesis and pharmacological activity of 2S-Verapamil, S,S-Ethambutol.
10. Synthesis and pharmacological activity of (+)Lomefloxacin, Fluvastatin.
11. Synthesis and pharmacological activity of Dextropropoxyphen, (+)Ephedrine.
12. Synthesis and pharmacological activity of (+)Griseofulvin, Dexormaplatin.
13. Synthesis and pharmacological activity of R-Indacrinone, Nateglinide.
14. Synthesis and pharmacological activity of Oxybutynin hydrochloride.
15. Synthesis and pharmacological activity of S,S- Captopril and S,S,S- Enalaprilate
Course/Paper - IV
CH(CPI)404 T (ELECTIVE-IIIA) Advanced Heterocyclic Chemistry
Unit: CPI - 49: Non aromatic heterocyclics & Aromaticity
Topics to be covered No. of Hours
required
Different types of strains, interactions and conformational aspects of non-
aromatic heterocycles
1
Synthesis, reactivity and importance of Azirines, Aziridines 2
Synthesis, reactivity and importance of Oxiranes, Oxaziridines 2
Synthesis, reactivity and importance of Diazirenes, Diaziridines 2
Synthesis, reactivity and importance of Thiiranes, Azetidines 2
Synthesis, reactivity and importance of Oxetanes, thietanes 2
Aromaticity introduction, Aromatic and anti aromatic compounds, Criteria
for aromaticity
1
Huckel’s 4n+2 electron rule for benzene and non benzenoid aromatic
OC(CB3)-28: Total stereoselective synthesis of natural products. Dr.A.Krishnam Raju
1. Introduction and importance of stereoselective total synthesis of natural products.
2. Importance of Dynemicin A and Plan of synthesis
3. Synthesis of Dynemicin A
4. Importance of Prostaglandins, Classification and nomenclature of Prostaglandins
5. Corey’s synthesis of prostaglandins E2
6. Corey’s synthesis of prostaglandins F2α
7. Corey’s synthesis of paeoriflorin
8. Introduction to Carbohydrates: Family of Aldohexoses: Writing the stereochemical
structures of D-hexoses.
9. Sharpless synthesis of L-hexoses
10. Importance and Isolation of Taxol
11. Nicolaous synthesis of taxol
12. Importance of indolizomycin
13. Danishefsky synthesis of indolizomycin
14. Importance and Takasago synthesis of menthol
15. Importance and Hoffmann-LaRoche synthesis of Biotin
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Paper IVB OC(CB4)-29 : Pharmacokinetics
Unit: Pharmacokinetics.
No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Introduction and importance of ADME studies of drugs 1
. Routes of administration . i)Absorption: Definition, absorption of drugs across the membranes
1
Physico chemical factors affecting the drug absorption (emphasis on pH partition hypothesis and Drug Dissolution).
1
Methods of determination of drug absorption 1
Methods of determination of drug absorption 1
Bioavailability. ii)Distribution: Apparent volume of drug distribution. 1
Factors affecting distribution, plasma protein binding. 1
iii) Metabolism: Sites of drug metabolism, 1
metabolic rate constant, bioactivation
1
biotransformation of drugs ( phase I and phase II reactions) 1
iv)Elimination: Types of elimination 1
overall apparent elimination rate constant 1
and half-life, concept of clearance 1
Over view of the topic 1
Seminar by students 1
15hrs
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Paper IVB OC(CB4)-29: Pharmacodynamics.: Organic Chemistry,
Unit: Pharmacodynamics. No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Introduction 1
targets for drug action, receptor concept 2
Pharmacological binding terms 1
Twostatereceptor model, 1
, receptor families- structure and signal transduction mechanisms 1
channel linked proteins, gating mechanism,.
2
G-protein coupled receptors 1
G-protein and their role, 1
Targets for G-proteins, Kinase linked receptors 1
, receptors that regulate gene transcription. 1
. Theories of concentration -response relationship 1
. Theories of concentration - dose-response curves 1
Over view of the topic 1
15hrs
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Course/Paper: IVB
Unit: OC(CB4)-30: Principles of Therapeutics No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
1. Introduction 1
Plasma Drug concentration vs Time profile,Definition and explanation of various terms: MEC, MSC, MTC, AUC(graph).
2
Peak plasma concentration, time of peak concentration Therapeutic range 2
Steady state concentration, onset of action, onset of time, duration of action, intensity of action. LD50, ED50. Therapeutic objective.
1
Dosage regimen, Design of dosage regimes: Dose size, dosing frequency, drug accumulation during multiple dosing, time to reach steady-state during multiple dosing, average concentration and body content on multiple dosing to steady state
2
loading dose, maintenance dose, maintenance of drug within the therapeutic range, 1
design of dosage regimen from plama concentration. 1
Kinetics of fixed dose, fixed time interval regimes. 1
Modification to dosage regime: 1
Dosing of drugs in obese patients, dosing of drugs in Neonates, infants & children 2
dosing of drugs in geriatrics (elderly), dosing of drugs in Hepatic disease, dosing of drugs in renal disease.
2
overview 1
15hrs
NIZAM COLLEGE : DEPARTMENT OF CHEMISTRY
LESSON PLAN FOR THE ACADEMIC YEAR 2017-2018 (Semester IV)
Class : M. Sc final year Section: Organic Chemistry
Paper IVB OC(CB4)-31: Drug Interactions.
Unit: Drug Interactions.
.
No. of Hours Allotted: 15
Topics to be covered No. of Hours
required
Introduction 1
Introduction, classification, Mechanisms of drug interactions 1
pharmacokinetic interactions(alteration of gastrointestinal absorption, compexation and adsorption,
2
alteration of distribution, alteration of metabolism and alteration of excretion 1