Salbutamol SAR, synthesis_ By Ankita Vishe.pdf

This PowerPoint presentation provides a detailed overview of Salbutamol (Albuterol), a widely used bronchodilator for asthma and COPD. It covers therapeutic uses, the scheme of synthesis, and the structure-activity relationship (SAR), explaining how chemical modifications influence its pharmacological activity. Ideal for pharmacy students, researchers, and healthcare professionals, this PPT includes mechanism of action, synthesis pathway, and clinical applications. Enhance your knowledge of medicinal chemistry and drug design with this comprehensive resource.

1. Sympathomimetic agent

- SALBUTAMOL

E Presented by : Assigned by:
| Ankita Vishe Dr. Ujwala Tumbhe: : : : : :
| Roll no: 2413 2. ILIN!

een 5

2. CONTENTS

» Introduction

- Classification of Sympathomimetic agent
+ Structure & IUPAC name

+ Uses

» Adverse effect

- SAR (structure Activity Relationship)

« Mechanism of action

+ Scheme of synthesis

3. WHAT IS SYMPATHOMIMETIC AGENTS ? a

A sympathomimetic agent is a type of drug or
substance that mimics the effects of the sympathetic
nervous system (SNS). The SNS is part of the
autonomic nervous system that prepares the body for
"fight or flight" responses during stress or
emergencies.

4. CLASSIFICATION OF
SYMPATHOMIMETIC AGENT

01 02

5. STRUCTURE AND IUPAC NAME

wo
ey
HOW N”

[ 1-( 4 - hydroxy -3- hydroxylmethyl phenyl-2-
( tbutylamino) ethanol |

6. USES

To treat bronchial COPD ( chronic
obstructive pulmonary disorder )

0) To treat bronchial asthma

7. ADVERSE EFFECTS

increased heart Rash or swelling Dizziness
rate at injection site
Nervousn: ess Headache eight gain

8. SAR (STRUCTURE ACTIVITY RELATIONSHIP )

Epinephrine Salbutamol

+ Hydroxyl group in catechol at 3rd position is replaced by methylhydroxy
group which make salbutamol beta 2 selective.
+ Tertiary butyl group in salbutamol also increases beta 2 selectivity

9. MECHANISM OF ACTION

Salbutamol

Activates ß, receptors
in bronchial smooth
muscle

Activates adenylyl
cyclase activity

y

TcAMP

Smooth muscle
relaxation

Bronchodilatation

10. SCHEME OF SYNTHESIS

f i
HO: + CI—C—CH,CI ————> HO. C—CH,CI
Chloro acetyl
chloride

HOH,C HOH,C
o-Hydroxybenzyl
alcohol H¿NC(CHa)a

H

? i
1
—CH,NHC(CH,), HO C—CH,NHC(CH2
| ren
H MPV reduction

HOH,C
Salbutamol

11. THANK
YOU