Syllabus SyBP501T MEDICINAL CHEMISTRY – II (Theory)

 

BP501T          MEDICINAL CHEMISTRY – II (Theory)                                      3 L + 1T / Week

Scope: 

This subject is designed to impart fundamental knowledge on the structure, chemistry and therapeutic value of drugs. The subject emphasizes on structure-activity relationships of drugs, the importance of physicochemical properties and metabolism of drugs. The syllabus also emphasizes on the chemical synthesis of important drugs under each class.

Objectives: Upon completion of the course the the student shall be able to

1.      Understand the chemistry of drugs with respect to their pharmacological activity

2.      Understand the drug metabolic pathways, adverse effect and therapeutic value of drugs

3.      Know the Structural Activity Relationship of different class of drugs

4.      Study the chemical synthesis of selected drugs

 

Sr. No.	Content: 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 (*)	Hours
1	UNIT I	10
1.1	Antihistaminic agents: Histamine, receptors and their distribution in thehumanbody 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.	4
1.2	Gastric Proton pump inhibitors: Omeprazole, Lansoprazole, Rabeprazole,Pantoprazole	1
1.3	Anti-neoplastic agents: Alkylatingagents: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.	5
2	UNIT II	10
2.1	Anti-anginal: Vasodilators: Amyl nitrite, Nitroglycerin*, Pentaerythritol tetranitrate, Isosorbidedinitrite*, Dipyridamole. Calcium channel blockers: Verapamil, Bepridil hydrochloride, Diltiazemhydrochloride, 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	7
2.2	Anti-hypertensive Agents: Timolol, Captopril, Lisinopril, Enalapril, Benazeprilhydrochloride, Quinapril hydrochloride, Methyldopate hydrochloride,* Clonidine hydrochloride, Guanethidine monosulphate, Guanabenz acetate, Sodium nitroprusside, Diazoxide, Minoxidil, Reserpine, Hydralazine hydrochloride.	3
3	UNIT III	10
3.1	Anti-arrhythmic Drugs: Quinidine sulphate, Procainamide hydrochloride,Disopyramide phosphate*, Phenytoin sodium, Lidocaine hydrochloride, Tocainide hydrochloride, Mexiletine hydrochloride, Lorcainide hydrochloride, Amiodarone, Sotalol.	4
3.2	Anti-hyperlipidemic agents: Clofibrate, Lovastatin, Cholesteramine andCholestipol	2
3.3	Coagulant & Anticoagulants: Menadione, Acetomenadione, Warfarin*,Anisindione, clopidogrel	2
3.4	Drugs  used    in         Congestive      Heart  Failure:           Digoxin Digitoxin,Nesiritide, Bosentan, Tezosentan.	2
4	UNIT IV	08
4.1	Drugs acting on Endocrine system Nomenclature, Stereochemistry and metabolism of steroids	2
4.2	Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol,Oestrione, Diethyl stilbestrol.	1
4.3	Drugs for erectile dysfunction: Sildenafil, Tadalafil	1
4.4	Oral contraceptives: Mifepristone, Norgestril, Levonorgestrol	1
4.5	Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone,Dexamethasone	2
4.6	Thyroid and antithyroid drugs: L-Thyroxine, L-Thyronine, Propylthiouracil,Methimazole.	1
5	UNIT V	07
5.1	Antidiabetic agents: Insulin and its preparations Sulfonyl ureas: Tolbutamide*, Chlorpropamide, Glipizide, Glimepiride. Biguanides: Metformin. Thiazolidinediones: Pioglitazone, Rosiglitazone. Meglitinides: Repaglinide, Nateglinide. Glucosidase inhibitors: Acrabose, Voglibose.	2
5.2	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.*	5
	Total	45

Reference Books (Latest Editions to be adopted)

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.