Background:
Approach for green chemistry for chemical synthesis is found to be very efficient
as it makes the reaction more easily, less tedious, maximize desired products and minimize
by-products.
Materials & Methods:
Utilizing this approach 1, 5-benzodiazepines and its derivatives have been
synthesized and evaluated for skeletal muscle and antianxiety activity. 1, 5-benzodiazepine derivatives
have attracted great attention due to its diversity of pharmacological activities and its application
in heterocyclic synthesis and medicines. The target compounds were synthesized by first reacting
o-phenylenediamine with acetophenone to yield 1, 5-benzodiazepines. In the next step the NH of
1, 5-benzodiazepines were chloroacetylated and then the chloro group was substituted with different
anilines. The structures were confirmed on the basis of their TLC, IR, 1H NMR and CHN elemental
studies. The physicochemical parameters were determined for BBB penetration through online software.
Results:
The Log P values of the compounds tested showed that compounds have the potential to be
CNS active. The compounds were evaluated for the skeletal muscle relaxant activity and antianxiety
activity. It was investigated that 1, 5-benzodiazepines derivatives possess significant differences between
control group and treated group.
Conclusion:
Among these derivatives, the compound bearing chloro group possesses the highest
skeletal muscle relaxant and antianxiety activity.
DEVELOPMENT AND PROCESS OPTIMIZATION OF SOLID DOSAGE FORM (SKELETAL MUSCLE RELAXANT) FROM LAB SCALE TO PILOT SCALE
