BP501T. MEDICINAL CHEMISTRY – II Books
“Medicinal Chemistry II: Exploring the design, synthesis, and optimization of pharmaceuticals. Delve into advanced topics in drug discovery, including structure-activity relationships, pharmacokinetics, and pharmacodynamics. Investigate case studies of successful drug development and current trends in medicinal chemistry research.”
Course Content
Unit Title
Content
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: Amylnitrite, 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, Ethacrynicacid.
PotassiumsparingDiuretics: 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 onEndocrinesystem Nomenclature,Stereochemistryand metabolism of steroids
Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethylstilbestrol. - 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
BenzoicAcidderivatives;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.*
Learning Objectives
- Understand the chemistry of drugs with respect to their pharmacological activity
- Understand the drug metabolic pathways, adverse effect and therapeutic value of drugs
- Know the Structural Activity Relationship of different class of drugs
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