|SAR of benzodiazepines|
- Electronegative substitution at 7 increase activity.
- 6,8 or 9 substitution- decrease activity.
- Proton accepting group at 2 must for benzodiazepine.
- 3-OH/ 3-COOR has no effect increase excretion.
- N1 has no effect but sterically bulky substituent can decrease activity.
- C=N if changed to C-N decrease activity.
- 4' substitution- Decrease activity ( Steric limitations).