Background: Anxiety and oxidative stress are the common disorders prevailing in the modern
age. Many new pyrazoline derivatives have been synthesized and patented, but there is still continuous
research in progress to explore antidepressant and antioxidant potential of pyrazoline scaffold.
Objectives: The present work was carried out to synthesize, characterize and evaluate the pharmacological
potential of 1,3,5-Pyrazoline derivatives.
Methods: Ten new 1,3,5-Pyrazoline derivatives were synthesized and characterized by IR, 1HNMR
and mass spectral techniques. The synthesized pyrazoline derivatives were investigated for their
in vivo antidepressant activity by Tail Suspension Test (TST) and in vitro antioxidant activity by
FRAP and DPPH assay methods. The docking studies and in silico ADME and toxicity characteristics
were also evaluated.
Results: Among the synthesized analogues, IVh showed the highest antidepressant activity with a significant
reduction in the duration of immobility. The compound IVh emerged as the most potent antioxidant
compound due to the presence of an electron releasing hydroxyl group. Docking studies of
most potent compounds revealed good interaction points with the MAO-A enzyme. The compounds
were found to obey Lipinski’s Rule of Five and displayed the least in silico toxicity profile.
Conclusion: The synthesized compounds were found to possess great potential in decreasing the duration
of immobility in Swiss albino mice and scavenging free radicals. These compounds may serve as
new leads for further drug exploration.