LUQMAN COLLEGE OF PHARMACY, GULBARGA

 

MEDICINAL CHEMISTRY-II – 4Th B-Pharm (75 Hours)

 

First Sessional

 

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Chapter No

Topic

Sub Topic

Hours

01.

Chapter No-01

Modern concept of rational drug design:

A) A brief introduction to quantitative structure activity relationship (QSAR), Prodrug, Combinatorial Chemistry and Computer Aided Drugs Design.(CADD).

B) History and development of chemotherapeutic agents: Structure,uses and synthesis of only those compounds that are underlined and superscribed by ‘s’

c) Anti-infective agents:

1. Local anti-infective agents:

a) Alcohols and related compounds: Alcohol,isopropyl alcohol,formaldehyde soloution.

b) Phenols and their derivatives:p-Chloro phenol, hexachlorophene, Resorcinol, hexyl resorcinol.

c) Oxidizing agents: Hydrogen peroxide soloution, hydrous benzoyl peroxide.

d) Halogen containing compounds: Iodine tincture, Chlorine containing compounds-halozone.

e) Cationic surfactants:Benzalkonium chloride, cetylpyridinium chloride.

f) Dyes-Gentain Violet, Methylene blue.

g) Nitrogen compounds: Nitrofurazone, Furazolidone.

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02.

Chapter No-02

Preservatives

a) Para hydroxy benzoic acid derivatives: Methylparben, Propyl paraben, Ehtyl paraben.

b) Miscellaneous: Chlorobutanol, Benzyl alcohol, Phenylethyl alcohol, Sodium benzoate, Phenyl mercuric nitrate, Phenyl mercuric acetate.

 

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03.

Chapter No-03

Antifungal agents

a) Antifungal antibiotics-Nystain, Candicidin, Hamycin, Griseofulvin Ampoterecin-B.

Synthesis anti fungal agents

b) Substituted imidazoles: Clotrimazole, Miconozole, Ketoconazole.

c) Miscellaneous –Zinc propionate, Sodium caprylate, Tolnaftate.

 

 

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04.

Chapter No-04

Urinary tract anti-infectives

a) Quinolones: Nalidixic acid, Cinoxacin, Norfloxacin, Ciprofloxacin, Pefloxacin, Ofloxacin, Sparfloxacin.

b) Miscellaneous : Nitrofurantoin.

 

(02 Hours)

05.

Chapter No-05

Antiubercular drugs: SAR of antiubercular drugs,

a) Synthesis antiubercular agents: p-Aminosalysilic acid, Isoniazid, Ethambutols, Pyrazinamide, Ethionamide, Clofazimine.

b) Antiubercular Antibiotic: Cycloserine, Viomycin sulfate, Capreomycin sulfate, Rifampicin.

 

 

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06.

Chapter No-06

Anti viral agents

a) Amantidine hydrochloride, Iodoxuridine, Zidovudine.

b) Anti-AIDS: Aza thymidine, Suramin.

 

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07.

Chapter No-07

Antiprotozoal agents

Emetine hydrochloride, Metronidazole, Diloxanide furoates, 8-hydroxy Quinoline derivatives ( clioquinal, iodoquinal), Carbarsone.

 

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08.

Chapter No-08

Anthelmintics

Piperazine, Diethyl carbamazine, Pyrantel pamoate, Thiabendazole, Mebendazole,

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Second Sessional

 

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Chapter No

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D) Sulfonamides, Sulfones as antibacterial agents:

1. SAR of Sulfonamides.

2. Classification of sulfonamides based on duration of action with example. Sulfamethiazole, Sulfisoxazole, Sulfapyridine, Sulfamethoxazole, Sulfadiazine, Sulfacetaminde, Sulfasalazine, Phthalyl Sulfathiazole.

3. Folate reductase inhibitors: Trimethoprim, Synergistic action of the combination of Sulfamethoxzole and trimethoprim.

4. Sulfone : Dapsone.

E) Antimalarials : Ethiology of malaria, Histroy, Mechanism and SAR.

1. Quinolines and analogues: 7-chloro-4-amino quinolines: Chloroquine phosphates, Hydroxy Chloroquine. Sulphate,Amodiaquine. 8-amino quinolines: Pamaquine Primaquines, 9-amino acridines: Quinacrines.

2. Miscellaneous: Mefloquine, Pyrimethamine, Trimethoprine.

3. Biguanides and Dihydrothiazines:Chloroguanide, Cycloguanil.

F) Antibiotics: Historical background, Mechanism of action, classification.

1. Beta lactam antibiotic: Pencellins- Structure, chemical degradation bacterial resistance Penicillin G, Penicillin V, Cloxacillin sodium, Naficillin sodium, Ampicillin, Amoxcyllin.

2. Beta lactamase inhibitors: Clavulanic acid and  its salt, Thienamycin.

3. Cephalosporins: Structure and uss of Cephalexin, Cephradine, Cefadroxil, Cefixime, Cefapyridine, Cefutroxime.

4. Monolactams: Sulfazecin, Aztreonam, Tigmonam.

5. Aminoglycosides: Structural features and Mechanism of action, Streptomycin, Amikacin neomycin, Kanamycin, Gentamycin, Netilmycin.

6. Teracyclines: Chemistry and SAR, tetracycline, chloretracyline, Methacycline, Demeclocycline, Oxytetracycline, Meclocycline, Doxycycline, Minocycline.

7. Macrolide: Structure and specific uses of Erthromycin, Azithrocin, Oleandomycin.

8. Lincomycins:Lincomycin, Clindamycin.

9. Polypeptides: Gramicidin, Bacitracin, Polymyxin B, Colistin.

10. Miscellaneous: Chlormphenicol, Vancomycin, Novobiocin.

I.) Diuretics: Introduction

1) Carbonic anhydrase inhibitors: Acetazolamide, Methazolamide.

2) Thiazide and Thiazide like diuretics: Chlorthiazides, Benzthiazide, Xipamide, Chlorthaildone.

3) High-ceiling or loop diuretics: Furosemide, Ethacrynic acid.

4) Potassium sparing diuretics: Spironolactone, Triampterene, Amiloride.

5) Miscellaneous: Mannitol.

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Third Sessional

 

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G) Antineoplastic agents : Introduction, mechanism, of action and classification with example.

1. Alkylating agents: Mechlorethamine, Cyclophosphamide, Melphalan, Chlorambucil, Busulfan, Lomustine.

2. Antimetabolities: Mercaptopurine, Thioguanine, 5-Flurouracil, Methotrexate,

3. Antibiotics: Dactinomycin, Bleomycin, Mitomycin, Streptozocin.

4. Plant Product: Etopside, Taxol, Camphothesin, Vincristine, Vinblastin.

5. Harmones: Dromostanalone, Megestrol.

6. Miscellaneous : Asparginase, Cisplatin, Hydroxy urea.

7. Immunotherapy:Interferon alpha 2a and 2b.

H) Cardiovascular agents:

1. Antianginal agents and vasodilators: Chemical structure and specific uses of Amyl nitrite, Nitroglycerine, Isosorbide dinitrate.

2. Calcium antagonists: Brief introduction of calcium channels and thir blockers, Chemical structure and uses of verapamil, Diltiazem, Nifedepine, Nimodepine, Felodepine Dipyridamole, Cyclandelate.

3. Antiarrythmics drugs: structure chemical name and classification of antiarrythmics with example.

Class-I membrane depressant drugs: Quinidine Procainamide, Phenytoin.

Class-II-Beta Adrenergic blocking agents, Tocainide, Propranolol.

Class-II- Repolarization prolongators, Bretylium, Amiodarone.

ClassIV- Clacium channel blocker, Diltiazem, Verapamil.

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09.

Chapter No-09

Antihypertensive agents

Beta-blockers: Propranolol. Timolol.

ACE inhibitors : Captopril, Enalapril.

Diuretics: Hydrochlorthiazide, Spiranolactone

Calcium channel blockers: Nifedipine, Felodepine, Amlodepine

a1-Antagonist : Prazocin.

A2-against: Clonidine, Guanithedine.

Miscellenous: Resprepine, Hydralazine, Minixidil.

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10.

Chapter No-10

Antihyperlipidemic agents:

Structure and specific uses.

Clofibrate, Lovastatin, Cholestramine, Colestipol.

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11.

Chapter No-11

Anticoagulants

Dicumorol, Warfarin, Phenindione.

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12.

Chapter No-12

Hypoglycemic agents

Sulfonyl vureas-Chlorpropamide. Acetohexamide, Glipizide.

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13.

Chapter No-13

Thyroid Hormones

L-Thyroxine, L-Thyroxine.

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14.

Chapter No-14

Antithyroid drugs

Propylthiouracil, Methimazole.

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