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1. Shashikesh
Shukla
Student Dr. KNMIPER

2. SAR Of
Benzodiazipines
SAR means structure
activity relationship

3. 1
2
3
4
56
7
8
9

4. 1.Electron withdrawing
group at position 7 is
essential for activity.ex
diazepam

5. 2. Replacement of benzene
ring with heterocyclic ring
resultated in compound
with higher activity.

6. 3. In ring B a methyl group
at nitrogen atom in first
position increase the
activity .ex diazepam

7. 4. Cabonyl group at
second position is
necessary for activity.

8. 5. Replacement of
hydrogen with hydroxy
group at position 3 result
in compuond with low
activity .
Oxazepam

9. 6. Saturation of double
bond at 4 - 5 position
reduce activity of
compound .

10. 7. A phenyl substitution at
position 5 is essential for
activity and replacement
with heterocyclic ring
gives compound with
suficient activity.

11. 8. Electronegative
substitution in ring C at
Ortho position or bother
Ortho position is good for
activity .

12. 9. Presence of tiazol ring
on alpha phase of
benzodiazipines will
result in compound with
more activity. Ex
alprazolam