Drug SAR ( Structure Activity Relationship)

This presentation is an introduction to Structure Activity Relationship of drug which help in getting knowledge for development of new drug.

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 2 nd 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.html

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 S o 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