The document discusses the structure-activity relationship (SAR) in drug development, explaining how the 3D structure of molecules influences their biological activity. It highlights examples including morphine, hydromorphone, and codeine, describing how slight chemical modifications can significantly affect drug potency. The presentation concludes that understanding SAR is crucial for enhancing the effectiveness of bioactive compounds.

1. BSBT-211
Bio-inorganic and Bio-organic Chemistry.
Topic- DRUG SAR
Submitted To- Dr. Vineet Sharma.
Submitted By- Rishabh Deshwal.
Enrollment No.- Asu2016010100127.
IBT 2nd SEMESTER
School of Biosciences.

2. Overview
• In this presentation we are going to understand the structure –
Activity relationship i.e. SAR .
http://sarshalombiblecenter.org/drugprogram

3. What is SAR ?
• SAR – It stands for Structure – Activity Relationship .
• It is basically defined as the relationship between the 3D structure
of molecules and their biological activity.
• The analysis of SAR enables the determination of the chemical
group responsible for evoking a target biological effect in any living
organism.

4. Importance of SAR :
• It is important because it allows to make modification of the effect of
or the potency of a bioactive compounds like drugs by changing its
chemical structures.

5. Lets try to understand the concept of Drug
Sar.
As we have understand the importance of Drug Sar in the above slide
now lets try to understand its concept more specifically.
Lets understand with an example of Morphine .

6. MORPHINE
• As we all know morphine is a pain medication which acts directly on the
CNS ( Central Nervous System) to reduce the feeling of pain.
• Morphine is the main active compound in opium, the juice obtained from
the seed pods of the poppy plant “ Papaver somniferum”.
https://pubs.acs.org/cen/coverstory/83/8325/8325morphine.h
tml

7. Hydromorphone
• Hydromorphone is used to treat moderate to severe pain.
• It belongs to group dihydro-morphin-one.
• Alteration : The oxygen is double bonded to carbon 6. The double bond
between carbons 7 and 8 has been reduced to a single bond, by adding
two hydrogen atoms.
• Effect: Increase in relative potency.

8. Morphine Hydromorphone
http://opiophilia.blogspot.com/2012/12/opiate-structure-
activity-relationship.html

9. Codeine
• Codeine is an opiate used to treat pain, as a cough medicine, and
for diarrhea. It is also found naturally in opium.
• Alteration : methyl group attached to the oxygen on carbon.
• Effect : Activity reduced to only 10% of morphine.

10. Morphine Codeine
http://opiophilia.blogspot.com/2012/12/opiate-structure-
activity-relationship.html

11. Story of Morphine and its analogues
S.No. Opiate Brand name drugs Alterations to
morphine
1. Morphine MS Contin _
2. Codeine Paramol, Tylenol 3 A
3. Hydromorphone Dilaudid, Palladone B, C
A. Addition of a methyl group to the oxygen on carbon 3.
Creates a methyl-3-ether linkage. Reduces potency.
B. Alcohol group (-OH) on carbon 6 oxidized to a double bonded ketone
(=O). Increases potency.
C. Hydrogenation (two H atoms are added) of double bond between carbons 7 and
8. Increases potency.

12. Conclusion
So we understand from this presentation is that making a slight change in
chemical structure of any drug can results in the activity of the drug.

13. References
http://opiophilia.blogspot.com/2012/12/opiate-structure-activity-relationship.html
https://www.drugs.com/codeine.html
https://www.drugs.com/mtm/hydromorphone.html
https://pubs.acs.org/cen/coverstory/83/8325/8325morphine.html