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Synthesis, Docking and Anti-Inflammatory Activity of Triazole Amine Derivatives as Potential Phosphodiesterase-4 Inhibitors

[ Vol. 16 , Issue. 1 ]

Author(s):

Ajmer Singh Grewal, Viney Lather, Deepti Pandita and Ruchi Dalal   Pages 58 - 67 ( 10 )

Abstract:


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 disorders.

Keywords:

Anti-inflammatory activity, camp, docking studies, PDE4B, PDE4 inhibitors, triazole derivatives.

Affiliation:

Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Barnala Road, Sirsa, 125055, Haryana, Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Sirsa, 125055, Haryana, Department of Pharmaceutics, JCDM College of Pharmacy, Barnala Road, Sirsa, 125055, Haryana, Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Barnala Road, Sirsa, 125055, Haryana

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