Background: Pyrazolines are reported having anti-inflammatory, anti-oxidant and antidiabetic
activities in the literature. Drugs like celecoxib, antipyrine, etc. are structurally similar to the
Objectives: To synthesize and characterize N-acetyl pyrazole and quinoline conjugates and test them
for Anti-inflammatory, Antioxidant, Antibacterial, Antiamylase and Antimalarial activities.
Methods: A series of methoxy substituted quinoline based pyrazoline derivatives (2a-2j) were synthesized
in good to excellent yield from corresponding quinoline chalcones (1a-1j). The synthesized
compounds were characterized and screened for their in vitro anti-inflammatory, antioxidant,
antiamylase, antibacterial and antimalarial activities. Docking and in silico ADMET studies were
performed with PDB: 3LN1.
Results: Compounds 2b, 2i and 2j showed significant anti-inflammatory activity as compared to
standard sodium diclofenac. All compounds (2a-2j) showed excellent antioxidant activity for DPPH
even more than standard ascorbic acid. Compounds 2e, 2f, 2h and 2i showed excellent antioxidant
activity for NO. as compared to standard ascorbic acid. Compound 2f showed significant antioxidant
activity for SOR. Almost all the compounds showed significant antibacterial as well as anti-amylase
activity with few exceptions, whereas compounds 2f, 2h and 2j showed potent antimalarial activity.
Conclusion: Compounds have shown good anti-inflammatory activities as compared with diclofenac.
All the synthesized pyrazoline derivatives showed excellent anti-amylase activity as compared
to standard acarbose. Also, compounds have shown good antioxidant antibacterial and antimalarial