SET 2

Q. I ] Answer the following (Attempt any 1 out of 2) (8M)

1) A) Answer the following - 4M
i) Indicate the important functional groups in catecholamines (structures
needed) involved in binding to the adrenergic receptors.
ii) State the effect of introducing a bulky N-alkyl group on the amine nitrogen
of catecholamines with respect to their adrenergic activity
iii) Predict the effect of introducing substitutions on the side chain linking the
aromatic ring to the amine of catecholamine adrenergic agents.
iv) Write the structure of an aryloxy propanolamine analogue that is a β-
adrenergic blocker.
B) Identify the following drug, indicate its mechanistic class and outline its synthesis. 4M

2) A) Discuss in detail the structure-activity correlations within the benzodiazepine 4M

class of compounds for their hypnotic and sedative properties.
B) Identify the following anti-inflammatory agent. Indicate to which chemical class it 4M
belongs. Discuss the stereochemistry of the compound and draw the structure of its
active metabolite.
 SET 2

Q. II ] Answer the following (Attempt any 4 out of 5) (32M)

A) Explain why acetylcholine is a poor therapeutic agent. Outline the structural
modifications in acetylcholine which resulted in therapeutically useful drugs 4M
1) with agonistic activity at the muscarinic receptor.
B) What is the difference between ephedrine and pseudoephedrine in terms of
their structures, stereochemistry and mechanism of action? 4M

The following is a list of sympathomimetic agents. Classify them on the basis of

2) their chemical class and selectivity profile, draw the structures and give their 8M
therapeutic uses: Terbutaline, Phenylephrine, Oxymetazoline, Clonidine
A) Outline the chemical classification of antipsychotic agents with at least one
example from each class. (structures needed) 4M
3) B) Write a short note on the ‘succinimides’ class of anticonvulsants and outline
the synthesis of Ethosuximide. 4M

A) Name the following and depict their structures:

i. Any two multicyclic opioid agonists 4M
ii. Any two Opioid-Based Antidiarrheals
B) Match the following:
4)

4M

A) Define Optical isomerism and explain the significance of stereochemistry in

medicinal chemistry giving suitable examples. 4M
5) B) Predict any two Phase-I metabolites for each of the following (draw
structures):Thioridazine and Diazepam. 4M