Medicinal Chemistry

1. A) Modern Concept of rational drug design: A Brief introduction to Quantitative Structure Activity Relationship (QSAR), Prodrug, Combinatorial chemistry and Computer aided drug design (CADD) and concept of antisense molecules
A study of the development of the following classes of drugs including SAR, Mechanism of action, synthesis of important compounds, chemical nomenclature, brand names of important marketed products and their side effects.

B) Anti-infective agents
a) Local anti-infective agents:
Alcohols: Isopropyl alcohol
Phenols: cresols, hexyl resorcinol
Cationic surfactants: Benzalkonium chloride, Cetylpyridinium bromide
Nitrofurans: Nitrofurazone, furazolidone.
b) Antifungal agents:
Azoles: miconazole, ketoconazole, fluconazole
Miscellaneous: Tolnaftate, Naftifine
Antifungal Antibiotics: Amphotericin, Nystatin, Griseofulvin
c) Urinary tract anti-infectives:
SAR of quinolone antibacterial agents, Norfloxacin, ciprofloxacin*, sparfloxacin, ofloxacin
d) Antitubercular agents:
Management of tuberculosis.
Synthetic anti TB agents: INH*, Pyrizinamide, Ethambutol,
Anti TB antibiotics: rifampin, capreomycin
e) Antiviral agents and Anti AIDS agents:
amantadine, acyclovir, trifluridine, zidovudine, stavudine
f) Antiprotozoal agents:
Introduction to protozoal diseases and causative organisms
Metronidazole, diloxanidefuroate, dehydroemetine, nifurtimox.
g) Antihelmentics:
Benzimidazoles: mebendazole, Albendazole
Piperazine, diethylcarbamazine, Ivermectin

2. A) Antibiotics
Historical background and classification of antibiotics
Beta lactam antibiotics: development of acid resistant and extended spectrum Penicillins. Penicillin G, ampicillin, amoxicillin, cloxacillin
Beta lactamase inhibitors: Clavulanic acid, thienamycin
Cephalosporins: cephelexin, cefadroxil, cefuroxime
Aminoglycosides: Streptomycin, neomycin, amikacin, gentamicin
Tetracylines: Chemistry and SAR of tetracylines, chlortetracycline, doxycycline, Minocycline
Macrolides: Erythromycin, Azithromycin
Miscellaneous: Clindamycin, Bacitracin, Chloramphenicol*
B) Antineoplastic agents
Historical background and classification of antineoplastic agents
Alkylating agents: cyclophosphamide, mechlorethamine, cholrambucil
Antimetabolites: mercaptopurine, flurouracil, methotrexate
Antibiotics: dactinomycin, mitomycin, streptozocin
Plant products: etoposide, taxol, vincristine and vinblastine
Miscellaneous: cisplatin, interferons

3. A) Antimalarials
Etiology of malaria, SAR and mechanism of action of quinoline
Antimalarials
Quinine sulphate, Chloroquine phosphate, amodiaquine, pamaquine*, primaquine, Quinacrine
Chloroguanide, cycloguanil, pyrimethamine
B) Sulphonamides and sulphones
History and development of sulfonamides, SAR and mechanism of action of Sulfonamides,pKa of Sulfas and Crystalluria
Sulfamethoxazole, sulfisoxazole, sulfacetamide*, sulfasalzine
Folatereductase inhibitors: trimethoprim*, synergistic action of cotrimoxazole.
Sulfones: dapsone
C) Hypoglycemic agents
History, development and SAR of sulfonylureas: tolbutamide*, chlorpropamide, glipizide
Metaglinides: repaglinide
Thiazolindiones: rosiglitazone, pioglitazone
Biguanides: metformin, phenformin
Miscellaneous: acarabose, miglitol

4. A) Cardiovascular agents
a) Antianginal agents and vasodilators
Nitrovasodilators: amyl nitrite, Isosorbidedinitrate
Calcium Channel Blockers: Verapamil, Diltiazem
b) Antiarrhythmic agents:
Class I: quinidine, phenytoin, lidocaine, enacinide
Class II: beta blockers-propranolol
Class III: Amidoarone
Class IV: Calcium channel blockers: verapamil, diltiazem
c) Antihypertensive agents:
betablockers: Propranolol*
ACE inhibitors: captopril, enalapril
Angiotensin antagonists: losartan
Calcium channel blockers: nifedipine, amlodepine
Adrenergic agents: clonidine, methyl dopa
Adrenergic antagonists: prazosin, reserpine
d)Antihyperlipidemic agents: types of hyperlipoproteinemia
clofibrate, fenofibrate, cholestyramine, lovastatin, simvastatin
e)Anticoagulants: warfarin, dicumarol, anisindione

Diuretics
Carbonic anhydrase inhibitors: acetazolmide*
Thiazide diuretics: SAR of thiazide diuretics, chlorthiazide, benzthiazide, xipamide, chlorthalidone
Loop diuretics: frusemide*, ethacrynic acid
Potassium sparing diuretics: spiranolactone,amiloride
Miscellaneous: mannitol

5. A) Steroidal Hormones and Adrenocorticoids
Estrogens: estradiol, DES
Progestines: progesterone, norethindrone
Testosterone, nandralone
Betamethasone, prednisolone, beclomethasone
B) Thyroid and Antithyroid agents
L-thyroxine, l-threonine
Propyl thiouracil, methimazole
C) Diagnositc agents
Iodipamide, Diatriazoate sodium
Aminohippurate, sulfobromphthalein, fluorescein sodium