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Medicinal chemistry-lll

          MEDICINAL CHEMISTRY-III

STUDY OF classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted by (*) 

UNIT – I 

Antibiotics 

Historical background

Nomenclature 

Stereochemistry

Structure activity relationship

Chemical degradation 

Classification and important products of the following classes.

 β-Lactam antibiotics: 

Penicillin

Cepholosporins

β- Lactamase inhibitors

Monobactams 

Aminoglycosides: 

Streptomycin

Neomycin

Kanamycin 

Tetracyclines: 

Tetracycline

Oxytetracycline

Chlortetracycline

Minocycline

Doxycycline 

" MC III 60 MCQs with ANSWERS " 

UNIT – II

Antibiotics 

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. 

Antimalarials: Etiology of malaria

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 

Synthetic anti tubercular agents: 

Isoniozid*

Ethionamide 

Ethambutol 

Pyrazinamide 

Para amino salicylic acid* 

Anti tubercular antibiotics: 

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: 

Antifungal antibiotics:

Amphotericin-B 

Nystatin 

Natamycin 

Griseofulvin. 

Synthetic Antifungal agents: 

Clotrimazole

Econazole

Butoconazole

Oxiconazole 

Tioconozole 

Miconazole*

Ketoconazole

Terconazole

Itraconazole

Fluconazole

Naftifine hydrochloride

Tolnaftate*

Anti-protozoal Agents: 

Metronidazole*

Tinidazole

Ornidazole

Diloxanide

Iodoquinol

Pentamidine Isethionate

Atovaquone

Eflornithine

Anthelmintics: 

Diethylcarbamazine citrate*

Thiabendazole

Mebendazole*

Albendazole

Niclosamide

Oxamniquine

Praziquantal

Ivermectin

Sulphonamides and Sulfones 

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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