Title:Anti-inflammatory Activity of Pyrazole Analogues Deduced from Bioactive
Piperine: Synthesis, In silico, and In vitro Evaluation
Volume: 19
Issue: 2
Author(s): Lilbet Mathew, Murugesan sankaranarayanan and Ilango Kaliappan*
Affiliation:
- Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM Institute of Science and Technology
(SRMIST), Kattankulathur, 603 203, Chengalpattu (Dt), Tamil Nadu, India
Keywords:
Arachidonate-12-lipoxygenase, pyrazoline, pyrazolidine, HRBC membrane stabilization, molecular docking, NSAIDs, FTIR.
Abstract:
Background: Around ten novel pyrazoline and pyrazolidine derivatives were designed and
synthesized by the condensation of piperine, hydrazine hydrate, phenylhydrazine, aromatic carboxylic
acid, and ethanol.
Methods: The synthesized compounds (2, 3, 4a-d, and 5a-d) were characterized by FTIR, 1HNMR,
mass spectral, and elemental analysis. Pharmacokinetic, physicochemical, drug-likeness, and medicinal
chemistry friendliness parameters were also predicted by in silico methods.
Results: Furthermore, compounds were screened for in vitro anti-inflammatory activity by the HRBC
membrane stabilization method using diclofenac sodium as the standard drug. The tested compounds
showed moderate anti-inflammatory activity compared to the standard drug. The molecular docking
studies of significantly active (4d) and least active compounds (5d) were also carried out in the active
sites of an arachidonate-12-lipoxygenase target in order to study the putative binding pattern of the
study compounds.
Conclusion: According to the findings of this study, further lead identification as well as lead optimization
techniques will be required in the near future in order to get potent analogues.