UNIT – I
- Historical background
- Nomenclature
- Stereochemistry
- Structure activity relationship
- Chemical degradation
- Classification and important products of the following classes.
- Penicillin
- Cepholosporins
- β- Lactamase inhibitors
- Monobactams
Aminoglycosides:
- Streptomycin
- Neomycin
- Kanamycin
Tetracyclines:
- Tetracycline
- Oxytetracycline
- Chlortetracycline
- Minocycline
- Doxycycline
UNIT – II
- Historical background
- Nomenclature
- Stereochemistry
- Structure activity relationship
- Chemical degradation
Classification and important products of
the following classes :-
- Macrolide: Erythromycin Clarithromycin, Azithromycin.
- Miscellaneous: Chloramphenicol*, Clindamycin.
- Prodrugs: Basic concepts and application of prodrugs design.
- Quinolines: SAR, Quinine sulphate, Chloroquine*, Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine.
- Biguanides and dihydro triazines: Cycloguanil pamoate, Proguanil.
- Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone.
UNIT – III
Anti-tubercular Agents
- Isoniozid*
- Ethionamide
- Ethambutol
- Pyrazinamide
- Para amino salicylic acid*
- Rifampicin
- Rifabutin
- Cycloserine
- Streptomycine
- Capreomycin sulphate
Urinary tract anti-infective agents
Quinolones:
- SAR of quinolones
- Nalidixic Acid
- Norfloxacin
- Enoxacin
- Ciprofloxacin*
- Ofloxacin
- Lomefloxacin
- Sparfloxacin
- Gatifloxacin
- Moxifloxacin
Miscellaneous:
- Furazolidine
- Nitrofurantoin*
- Methanamine.
Antiviral agents:
- Amantadine hydrochloride
- Rimantadine hydrochloride
- Idoxuridine trifluoride
- Acyclovir*
- Gancyclovir
- Zidovudine
- Didanosine
- Zalcitabine
- Lamivudine
- Loviride
- Delavirding
- Ribavirin
- Saquinavir
- Indinavir
- Ritonavir
UNIT – IV
Antifungal agents:
- Amphotericin-B
- Nystatin
- Natamycin
- Griseofulvin.
- Clotrimazole
- Econazole
- Butoconazole
- Oxiconazole
- Tioconozole
- Miconazole*
- Ketoconazole
- Terconazole
- Itraconazole
- Fluconazole
- Naftifine hydrochloride
- Tolnaftate*
- Metronidazole*
- Tinidazole
- Ornidazole
- Diloxanide
- Iodoquinol
- Pentamidine Isethionate
- Atovaquone
- Eflornithine
- Diethylcarbamazine citrate*
- Thiabendazole
- Mebendazole*
- Albendazole
- Niclosamide
- Oxamniquine
- Praziquantal
- Ivermectin
Historical development, chemistry, classification and SAR of Sulfonamides:
- Sulphamethizole
- Sulfisoxazole
- Sulphamethizine
- Sulfacetamide*
- Sulphapyridine
- Sulfamethoxaole*
- Sulphadiazine
- Mefenide acetate
- Sulfasalazine.
Folate reductase inhibitors:
- Trimethoprim*
- Cotrimoxazole
Sulfones: Dapsone*
UNIT – V
Introduction to Drug Design
Various approaches used in drug design.
Physicochemical parameters used in quantitative structure activity
relationship (QSAR) such as partition coefficient, Hammet’s electronic
parameter, Tafts steric parameter and Hansch analysis.
Pharmacophore modeling and docking techniques.
Combinatorial Chemistry:
Concept and applications
chemistry: solid phase and solution phase synthesis.
PRACTICAL
I Preparation of drugs and intermediates
1 Sulphanilamide
2 7-Hydroxy, 4-methyl coumarin
3 Chlorobutanol
4 Triphenyl imidazole
5 Tolbutamide
6 Hexamine
II Assay of drugs
1 Isonicotinic acid hydrazide
2 Chloroquine
3 Metronidazole
4 Dapsone
5 Chlorpheniramine maleate
6 Benzyl penicillin
III Preparation of medicinally important compounds or intermediates by Microwave
irradiation technique
IV Drawing structures and reactions using chem draw®
V Determination of physicochemical properties such as logP, clogP, MR, Molecular
weight, Hydrogen bond donors and acceptors for class of drugs course content
using drug design software Drug likeliness screening (Lipinskies RO5)
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. 1-5.
9. Indian Pharmacopoeia.
10. Text book of practical organic chemistry- A.I.Vogel.
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