Synthesis, Docking and Anti-Inflammatory Activity of Some Newer Triazole Derivatives as Potential PDE7 Inhibitors
Journal Title: Journal of Gynecology and Neonatal Biology - Year 2017, Vol 2, Issue 1
Abstract
Phosphodiesterase 7 (PDE7), one of the members of PDE family has been reported as potential therapeutic target involved in inflammation. The present work was designed to synthesize and evaluate the anti-inflammatory activity of some newer substituted triazole derivatives as potential PDE7 inhibitors. A series of substituted triazole derivatives was synthesized and evaluated by in silico studies to determine the binding interactions for the best-fit conformations in the binding site of the PDE7 protein. The selected compounds from in silico studies were evaluated further for their anti-inflammatory activity in the animal models. Amongst the synthesized molecules, compound 3 showed higher anti-inflammatory activity. The in vivo results showed accordance to that of in silico results. Most of the synthesized molecules were found to have drug-like properties as devised by Lipinski’s rule of five. These molecules can act as the starting hits for the design of safe, effective and orally bioavailable PDE7 inhibitors for the treatment of various inflammatory disorders.
Authors and Affiliations
Viney Lather
Keywords
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- EP ID EP350202
- DOI 10.15436/2575-808X.17.1392
- Views 99
- Downloads 0
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