BP501T. MEDICINAL CHEMISTRY – II

                                                              

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, importance of physico-chemical properties and metabolism of drugs. The syllabus also emphasizes on chemical synthesis of important drugs under each class.

Objectives

Upon completion of the course 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

Course Content

Study of the development of the following classes of drugs, Classification, mechanism of action, usesof 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                                                                                                                                                  10 Hours

Anti-histaminic 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

Anti-metabolites: Mercaptopurine*, Thioguanine, Fluorouracil, Floxuridine, Cytarabine, Methotrexate*, Azathioprine

Antibiotics: Dactinomycin, Daunorubicin, Doxorubicin, Bleomycin

Plant Products: Etoposide, Vinblastin sulphate, Vincristin sulphate

Miscellaneous: Cisplatin, Mitotane.

UNIT-II                                                                                                                                           10 Hours

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

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

UNIT- IV                                                                                                                                                  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 antithyroid drugs: L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole.

UNIT– V                                                                                                                                                           07 Hours

Anti-diabetic 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. 1 to 5.
  9. Indian Pharmacopoeia.
  10. Text book of practical organic chemistry – A.I.Vogel.

 

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