MEDICINAL CHEMISTRY – II

Study of the development of the following 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 (*) 

UNIT- I 

Antihistaminic agents: Histamine, receptors and their distribution in the humanbody 

H1–antagonists: Diphenhydramine hydrochloride*, Dimenhydrinate, Doxylamines cuccinate, Clemastine fumarate, Diphenylphyraline hydrochloride, Tripelenamine hydrochloride, Chlorcyclizine hydrochloride, Meclizine hydrochloride, Buclizine hydrochloride, Chlorpheniramine maleate, Triprolidine hydrochloride*, Phenidamine tartarate, Promethazine hydrochloride*, Trimeprazine tartrate, Cyproheptadine hydrochloride, Azatidine maleate, Astemizole, Loratadine, Cetirizine, Levocetrazine Cromolyn sodium 

H2-antagonists: Cimetidine*, Famotidine, Ranitidin. Gastric Proton pump inhibitors: Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole

Anti-neoplastic agents:

Alkylating agents: Meclorethamine*, Cyclophosphamide, Melphalan, Chlorambucil, Busulfan, Thiotepa 

Antimetabolites: Mercaptopurine*, Thioguanine, Fluorouracil, Floxuridine, Cytarabine, Methotrexate*, Azathioprine 

Antibiotics: Dactinomycin, Daunorubicin, Doxorubicin, Bleomycin 

Plant products: Etoposide, Vinblastin sulphate, Vincristin sulphate 

Miscellaneous: Cisplatin, Mitotane. 

UNIT – II 

Anti-anginal:

Vasodilators: Amyl nitrite, Nitroglycerin*, Pentaerythritol tetranitrate, Isosorbide dinitrite*, Dipyridamole. 

Calcium channel blockers: Verapamil, Bepridil hydrochloride, Diltiazem hydrochloride, Nifedipine, Amlodipine, Felodipine, Nicardipine, Nimodipine. 

Diuretics: 

Carbonic anhydrase inhibitors: Acetazolamide*, Methazolamide, Dichlorphenamide. Thiazides: Chlorthiazide*, Hydrochlorothiazide, Hydroflumethiazide, Cyclothiazide, 

Loop diuretics: Furosemide*, Bumetanide, Ethacrynic acid. 

Potassium sparing Diuretics: Spironolactone, Triamterene, Amiloride. 

Osmotic Diuretics: Mannitol 

Anti-hypertensive Agents: 

Timolol, Captopril, Lisinopril, Enalapril, Benazepril hydrochloride, Quinapril hydrochloride, Methyldopate hydrochloride,* Clonidine hydrochloride, Guanethidine monosulphate, Guanabenz acetate, Sodium nitroprusside, Diazoxide, Minoxidil, Reserpine, Hydralazine hydrochloride. 

UNIT- III 

Anti-arrhythmic Drugs: 

Quinidine sulphate, Procainamide hydrochloride, Disopyramide phosphate*, Phenytoin sodium, Lidocaine hydrochloride, Tocainide hydrochloride, Mexiletine hydrochloride, Lorcainide hydrochloride, Amiodarone, Sotalol. 

Anti-hyperlipidemic agents: 

Clofibrate, Lovastatin, Cholesteramine and Cholestipol 

Coagulant & Anticoagulants: Menadione, Acetomenadione, Warfarin*, Anisindione, clopidogrel 

Drugs used in Congestive Heart Failure: Digoxin, Digitoxin, Nesiritide, Bosentan, Tezosentan.

UNIT- IV

Drugs acting on Endocrine system

 Nomenclature, Stereochemistry and metabolism of steroids

Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethyl stilbestrol. 

Drugs for erectile dysfunction: Sildenafil, Tadalafil. 

Oral contraceptives: Mifepristone, Norgestril, Levonorgestrol 

Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone, Dexamethasone 

Thyroid and antithyroid drugs: L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole. 

UNIT – V

Antidiabetic agents: 

Insulin and its preparations 

Sulfonyl ureas: Tolbutamide*, Chlorpropamide, Glipizide, Glimepiride. Biguanides: Metformin. 

Thiazolidinediones: Pioglitazone, Rosiglitazone.

Meglitinides: Repaglinide, Nateglinide. 

Glucosidase inhibitors: Acrabose, Voglibose. 

Local Anesthetics: SAR of Local anesthetics 

Benzoic Acid derivatives; Cocaine, Hexylcaine, Meprylcaine, Cyclomethycaine, Piperocaine. 

Amino Benzoic acid derivatives: Benzocaine*, Butamben, Procaine*, Butacaine, Propoxycaine, Tetracaine, Benoxinate. 

Lidocaine/Anilide derivatives: Lignocaine, Mepivacaine, Prilocaine, Etidocaine. 

Miscellaneous: Phenacaine, Diperodon, Dibucaine.* 

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. 1to 5. 

9. Indian Pharmacopoeia. 10. Text book of practical organic chemistry- A.I.Vogel.