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Synthesis, Physicochemical, Computational and Biological Evaluation of Phenylurea Derivatives as CNS Agents
- Source :
- Central Nervous System Agents in Medicinal Chemistry. 21:157-164
- Publication Year :
- 2021
- Publisher :
- Bentham Science Publishers Ltd., 2021.
-
Abstract
- Background: A series of phenylurea derivatives were designed and synthesized, The target compounds were subjected to pharmacological studies. Various other parameters such as physicochemical properties, computational studies, and % similarity were also calculated. Materials and Methods: The synthesis of the target compounds has been carried out by reaction of Phenylurea with chloroacetyl chloride to afford 1-(2-chloroacetyl)-3-phenylurea, which further reacted with substituted anilines. All the reactions were monitored by TLC. All the target compounds were purified by recrystallization and characterized by spectroscopic methods. Physicochemical parameters and Log P values of the synthesized derivatives were also calculated. It identified compounds that have the prospect to cross the blood-brain barrier (BBB) and are CNS active. Skeletal muscle relaxant activity was also carried out using the Rotarod method. Results: The data of Log P indicated that the synthesized compounds have the potential to cross the BBB, so they are CNS active. Pharmacological activities of the derivatives showed that the compounds containing chloro group have moderate skeletal muscle relaxant activity. The test compounds possess significant differences between the control group and the treated group. Conclusion: The synthesized derivatives containing chloro group were found to be more potent when compared to standard drug Diazepam. Various others parameters studied revealed that the drug has the potency to cross the blood-brain barrier.
- Subjects :
- Drug
Recrystallization (geology)
Phenylurea Compounds
General Neuroscience
media_common.quotation_subject
Phenylurea Derivatives
Skeletal muscle
Chloroacetyl chloride
Combinatorial chemistry
Rotarod performance test
Structure-Activity Relationship
chemistry.chemical_compound
Neuropsychology and Physiological Psychology
Aniline
medicine.anatomical_structure
chemistry
Rotarod Performance Test
medicine
Animals
Molecular Medicine
Potency
Central Nervous System Agents
media_common
Subjects
Details
- ISSN :
- 18715249
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Central Nervous System Agents in Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....60d5e142ad081ee168f5671d669a0622
- Full Text :
- https://doi.org/10.2174/1871524921666210908145356