PHARMACEUTICAL CHEMISTRY - MEDICINAL-II Question Papers 4 A.U

Answer question no.1(compulsory) and any four of the remaining. All questions carry equal marks

1. Explain the importance of sterioisomerism in the biological activity of drugs giving suitable examples.

2. Classify Sulphonamides giving structure of important members. Write the SAR, mode of action and side effects. Explain the importance of Pka in the desigh of safer sulfa drugs.

3. Enumerate antileprotic agents giving structures of important drugs. Write the SAR and mode of action of sulfonates. Outline the synthesis of Clofazimine and Dapsone.

4. Classify antihypertensive giving structures of one drug for each class. Write the SAR of b-adrenergic blockers and ACE inhibitors. Outline the synthesis of any one important member.

5. (a) Explain about prodrugs and soft drugs giving examples.
(b) Write a brief note on:

• Chemotherapeutic index
• Superinfection

6. (a) Discuss the factors affecting absorption of drugs. (b) Write notes on antiamoebic agents.

7. Classify antimalarials giving examples write the SAR and mode of action of aminoqunolines. Outline the synthesis of Mepacrine.

8. Give an account of :

• Carbonic anhydrase inhibitors
• Aalkylating agents
• Cholinergic agonists

PHARMACEUTICAL CHEMISTRY-VI (MEDICINAL-II)

1. Physico-chemical properties and biological activity: Influence of partition coefficient, covalent bonding, hydrogen bonding, surface activity, redox potentials, chelation, enantiomers, and geometrical isomerism an biological activity.
2. Factors affecting adsorption, transport, distribution and elimination of drugs, protein binding of drugs.
3. Introduction to the concepts of prodrug, soft drugs and targeted drugs
4. Introduction to principles of chemotherapy, chemotherapeutic index, drug resistance, super infection.
A study of the classification, mode of action, uses and synthesis of specified members in each of the following categories.
5. Antiinfective agents: a) Ectoparasiticides: Lindane, pyrethrins, sulfurated compounds, benzyl benzoate (b) Antiseptics and disenfectants: alcohol, formaldehyde, recorcinol, hydrogen peroxide, benza;konium chloride, gentian violet, methyline blue and furazolidone.
6. Sulphonamides: sulfisoxazole, sulphamethazole and sullphathiozole.
7. Antimycobacterial agents: a) Antitubercular agents: PASA, isoniazid b) antileprotic agents: dapsone
8. Antihelmintics: diethyl carbamazine citrate, mebendazole, tinidazole, thiobendazole and pyrantel pamoate
9. Antimalarials: Chloroquine, primaquine, mefloquine, and pyremetnamine.
10. Antiamoebic agents: metronizadole, diloxanide, furoate, and carbarsone.
11. Antifungal agents: clotrimazole, Ketocanazole and tolnaftate.
12. Antiviral agents: acyclovir, zidovudine, idoxuridine and adamantine
13. Cytostatic agents: chlorambucil, cyclophospamide, lomustine, methotrexate, 5-flouro uracil and mercaptourine
14. Adrenergic drugs: Biosynthesis and metabolism of catecholamines, direct and indirect sympathomimetics, mode of action and structure activity relations, adrenergic blocking agents, synthesis of amphetamine, phenyl ethylamine and isoproterneol.
15. Cholinergic agents and anticholinesterases: Structural features of acetylcholine, cholinergic agonists, anticholinesterases, synthesis of carbachol, physostigmine, neostigmine and dicyclomine.
16. Diuretics: acetazolamide, furosemide, ethacrynic acid and hydrochlorthiazide.
17. Antihypertensives: methyl dopa, amlodipine, prazocin and propranolol.