Medicinal Chemistry II-Theory

Teacher

Dr. Gopal Krishna Padhy

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Core Courses

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Course Name : Medicinal Chemistry II

Code(Credit) : BPHT3101 (4-0-0)

 

Course Objectives

  • To expose students towards different chemical classes of drugs and their pharmacological activity.
  • To develop the linkage between organic molecules and their transformation to the drug molecule
  • To explain the mechanisms of action for representative drug classes.
  • To explain the relationship between drug’s chemical structure and it’s therapeutic properties.
  • To discuss the metabolic pathways, adverse effect and therapeutic indications of drug molecules.

Learning Outcomes

  • Students will be able to name and classify drugs according to their chemical nature and pharmacological action.
  • Students will be able to predict the reactivity of organic compounds and their possible transformation in to drug molecules.
  • Students will be able to recognize and explain the types of molecular interaction between drugs and their biological target.
  • Students will be able to explain the relationship between drug’s chemical structure and it’s therapeutic properties.
  • Students will be able to know the metabolic pathways, adverse effect and therapeutic indication of drugs.

Course Syllabus

Module- I

Antihistaminic agents: Histamine, receptors and their distribution in the Human body

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.

Module– 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.

Module- 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.

Module- 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.

Module – 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.

Session Plan

Session 1

Antihistaminic agents: Classification of Antihistaminics

Case Studies

Case Studies

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