Activity 9

Structural Activity of Active Ingredients in a Formulation

OBJECTIVE
1. To compare the SAR of the active ingredient of two antidandruff shampoos.
2. To draw the structural formula of the active ingredients.

MATERIALS
Antidandruff shampoo

INSTRUCTIONS
Bring an antidandruff shampoo and note the ingredients on the back of the
packaging. List the active ingredients of each shampoo and draw the structural
formula of each active ingredient. Rationalize the difference in activity in terms of
structural activity.
 Activity 9
Structural Activity of Active Ingredients in a Formulation

Name:________________________________ Group No.___________

Course Year & Section:___________________

References:
 Activity 10
Structural Activity of Beta Lactam Antibiotics

OBJECTIVE
1. To discuss the structural activity of the given beta-lactam antibiotics.
2. To draw the beta-lactam ring.
3. To evaluate the pharmacological behavior of the given beta-lactam antibiotics.

MATERIALS
Drug leaflets of the following:
1. Amoxicillin
2. Cefalexin
3. Oxacillin
4. Cloxacillin

INSTRUCTIONS
Bring drug leaflets of the above-mentioned beta-lactam antibiotics per group. List the
pharmacokinetic and pharmacodynamic parameters of each antibiotic and separately
draw the beta-lactam ring as the parent structure (center circle) and the substituents
(guided with an arrow, then drawn inside a circle). Write the structural formula of
each antibiotic. Evaluate, compare, and rationalize the structural differences
responsible for the pharmacological activity of the given antibiotics.
 Activity 10
Structural Activity of Beta Lactam Antibiotics

Name:________________________________ Group No.___________

Course Year & Section:___________________

1. Drawings

2. Pharmacokinetics and Pharmacodynamics Parameters (per antibiotics).

3. Write down the physical and chemical properties of each antibiotic.

4. What are the different indications and adverse reactions of each antibiotic?

5. Define the following terms: Pharmacokinetics, Pharmacodynamics, Bacteriostatic,

Bacteriocidal, Lysis, Half-life.

References:
 Activity 11
Structural Activity of Lipophilic Drug

OBJECTIVE
1. Identify the structure of lipophilic drugs.
2. To fragment the three different structural formulas.
3. To draw the. Structure of the fragmented lipophilic drug.
4. To classify each fragment according to lipophilicity and hydrophilicity.

INSTRUCTIONS
Give at least five lipophilic drugs and draw their structure.
Fragment and label the structure lipophilic or hydrophilic.

Guide questions
What are the properties of each chosen lipophilic drug?
Discuss the properties of lipophilic drugs. .

References:
 Activity 12
Structural Activity of Hydrophilic Drug

OBJECTIVE
1. Identify the structure of a hydrophilic drug.
2. To fragment the three different structural formulas.
3. To draw the. Structure of the fragmented hydrophilic drug.
4. To classify each fragment according to lipophilicity and hydrophilicity.

INSTRUCTIONS
Give at least five hydrophilic drugs and draw their structure.
Fragment and label the structure lipophilic or hydrophilic.

Guide questions
What are the properties of each chosen hydrophilic drug?
Discuss the properties of hydrophilic drugs.

References: