Medicinal Chemistry-II

Syllabus

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 (*)

Module 01                                                                                                                           10 Hours

Antihistaminic Agents

• Histamine, receptors and their distribution in the human body.
• H₁–Antagonists:Diphenhydramine hydrochloride*, Dimenhydrinate, Doxylaminescuccinate, 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.

Module 02                                                                                                                            10Hours

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.

Module 03                                                                                                                           10 Hours

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 and Anticoagulants

• Menadione, Acetomenadione, Warfarin*, Anisindione, clopidogrel.

Drugs used in Congestive Heart Failure

• Digoxin, Digitoxin, Nesiritide, Bosentan, Tezosentan.

Module 04                                                                                                                           08 Hours

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 Anti-Thyroid Drugs

• L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole.

Module 05                                                                                                                           07 Hours

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 Anaesthetics

• SAR of local anaesthetics.
• 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.*