Title:Synthesis, Physicochemical, Computational and Biological Evaluation of Phenylurea Derivatives as CNS Agents
Volume: 21
Issue: 3
Author(s): Shweta Verma and Sandeep Singh*
Affiliation:
- Faculty of Pharmacy, IFTM University, Lodhipur, Moradabad (UP) 244001,India
Keywords:
Phenylurea, aniline, skeletal muscle relaxant, rotarod, spectroscopic.
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.