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Glacial Acetic Acid Catalyzed Synthesis, Physicochemical and Biological Evaluation of Benzodiazepines as Potent CNS Agents
- Source :
- Central Nervous System Agents in Medicinal Chemistry. 19:146-151
- Publication Year :
- 2019
- Publisher :
- Bentham Science Publishers Ltd., 2019.
-
Abstract
- 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.
- Subjects :
- Green chemistry
Anxiety
Chemical synthesis
Catalysis
Benzodiazepines
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Acetic acid
medicine
Animals
Organic chemistry
Maze Learning
Acetic Acid
Muscle Relaxants, Central
Chemistry
General Neuroscience
Skeletal muscle
Green Chemistry Technology
Neuropsychology and Physiological Psychology
medicine.anatomical_structure
Anti-Anxiety Agents
Proton NMR
CNS agents
Molecular Medicine
Central Nervous System Agents
Acetophenone
Subjects
Details
- ISSN :
- 18715249
- Volume :
- 19
- Database :
- OpenAIRE
- Journal :
- Central Nervous System Agents in Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....01d03f9f6c49f6b30343fdedfb4071f7
- Full Text :
- https://doi.org/10.2174/1871524919666190227234238