Background: Phosphodiesterase 4 (PDE4), is one of the members of PDE superfamily
which catalyzes the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate
in pro-inflammatory and immunomodulatory cells, leading to increased inflammatory
processes. PDE4 has been reported as an attractive therapeutic target involved
in various inflammatory disorders.
Objective: The present work was designed to synthesize and evaluate the anti-inflammatory
activity of some new triazole amine derivatives as potential PDE4 inhibitors.
Method: The present work involved the synthesis of a series of newer substituted triazole
amine derivatives followed by characterization using FTIR and 1H-NMR spectroscopy and
their in silico evaluation by docking studies to determine the binding interactions for the
best fit conformations in the binding site of PDE4 protein. Based on the results of the in
silico studies, the selected compounds were tested for the anti-inflammatory activity using
carrageenan-induced paw oedema method.
Results: The yields of synthesized compounds were moderate and amongst the synthesized
molecules, compound 5 demonstrated high anti-inflammatory activity. The results of experimental
studies were found to be in concordance with that of the in silico docking results.
Most of the synthesized molecules were also found to possess drug like properties as contrived
by Lipinski's rule of five.
Conclusion: These newly synthesized molecules could act as the starting hits for the design
of effective, potent and selective PDE4 inhibitors for the promising treatment of inflammatory