Introduction to Structure – Activity Relationship of Drugs – PST05106 Pharmaceutical Organic Chemistry

NTA Level 5 • Semester 1 • PST05106

Introduction to Structure – Activity Relationship of Drugs

Pharmaceutical Organic Chemistry • Source Session/Topic 25
Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability.

Session 25: Introduction to Structure – Activity Relationship of Drugs.

Total Session Time: 60 minutes

Prerequisites

None

Learning Tasks

By the end of this session students are expected to be able to:

• Define structure-activity relationship
• Explain the importance of structure-activity relationship in pharmacy

Resources Needed:

• Flip charts, marker pens, and masking tape
• Black/white board and chalk/whiteboard markers

SESSION OVERVIEW

|Step |Time |Activity/ |Content |

| | |Method | |

|1 |05 minutes |Presentation |Introduction, Learning Tasks |

|2 |10 minutes |Brainstorming |Definition of structure – activity |

| | |Presentation |relationship |

|2 |30 minutes |Group |Importance of structure – activity |

| | |discussion |relationship in pharmacy |

| | |Presentation | |

|4 |05 minutes |Presentation |Key Points |

| 5 |10 minutes |Presentation |Evaluation |

SESSION CONTENTS

STEP 1: Presentation of Session Title and Learning Tasks (5 minutes)

READ or ASK students to read the learning tasks and clarify

ASK students if they have any questions before continuing.

STEP 2: Definition of Structure – Activity Relationship (10 minutes).

|Activity: Brainstorming (5 minutes) |

| |

|Ask students to brainstorm on the following question: |

| |

|What is structure- activity relationship? |

| |

|ALLOW few students to respond. |

| |

|WRITE their responses on the flip chart/ board. |

| |

|CLARIFY and SUMMARISE by using the table below |

Structure Activity Relationship (SAR):

• A structure activity relationship relates features of a chemical

structure to a property, effect, or biological activity associated

with that chemical.

• SAR is the subject which brings about the awareness of the

relationships between the chemistry of a particular compound or group

of compounds and their interaction with the body hence activity.

STEP 3: Importance of Structure – Activity Relationship in Pharmacy (30

minutes).

|Activity: Small Group Discussion (15 minutes) |

| |

|DIVIDE students into small groups. |

| |

|ASK students to discuss in groups on the following questions. |

|What is the importance of structure- activity relationship in Pharmacy?|

| |

|[pic]REFER Students to Book |

| |

|ALLOW students to discuss for 10 minutes. |

| |

|ALLOW each group to present for 5 minutes. |

| |

|CLARIFY and SUMMARIZE by using the contents below |

• SAR enables the determination of the chemical groups responsible for

evoking a target biological effect in the organism.

• It allows modification of the effect or the potency of a bioactive

compound (typically a drug) by changing its chemical structure

• Medicinal chemists use the techniques of chemical synthesis to insert new

chemical groups into the biomedical compound and test the modifications

for their biological effects.

STEP 4: Key Points (05 minutes).

• The structure–activity relationship (SAR) is the relationship between

the chemical or 3D structure of a molecule and its biological activity.

• SAR enables the determination of the chemical groups responsible for

evoking a target biological effect in the organism.

• It allows modification of the effect or the potency of a bioactive

compound (typically a drug) by changing its chemical structure.

• Medicinal chemists use the techniques of chemical synthesis to insert new

chemical groups into the biomedical compound and test the modifications

for their biological effects.

STEP 5: Evaluation (10 minutes)

• What is Structure-activity relationship?
• What is the importance of SAR in pharmacy?

References

Ternay, A.L (1976). Contemporary Organic Chemistry. Philadelphia, United

States: W.B. Saunders Co.

Morrison R.T and Boyd R N (1997). Organic Chemistry (6th Ed.). New Delhi,

India: Prentice Hall of India

Graham Solomon et al (2014). Organic Chemistry (11th Ed.). New Jeysey,

United States: John Willey and Sons.

Nadendla R. R. (2005). Principles of Pharmaceutical Organic Chemistry. New

Delhi, India: MacMillan Publishers

Bruice Y (2013). Organic Chemistry (7th ed.). New York, United States:

Prentice Hall Pearson.

Delgado J. N. Et al (1998). Wilson and Gisvold's Textbook of Organic

Medicinal and Pharmaceutical Chemistry (10th Ed.). Calfornia, United

States: Lippincott Williams

Bhassin S.K, Gupta R. (2013). Pharmaceutical organic chemistry (E-book

Kindle edition). New Delhi, India: Elsevier Publishing Services

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