AI Article Synopsis
- Researchers synthesized and characterized oxadiazole derivatives (1-16) using H NMR, C NMR, and HREI-MS to evaluate their ability to inhibit thymidine phosphorylase.
- The derivatives showed varying inhibition levels (1.10 ± 0.05 to 49.60 ± 1.30 μM), with 7-Deazaxanthine as the standard for comparison (IC value 38.68 ± 1.12 μM).
- A structure-activity relationship (SAR) was established to analyze how different substitutions and functional groups on the phenyl ring affect inhibition, and molecular docking studies were conducted to explore binding interactions with the enzyme
Article Abstract
We have synthesized oxadiazole derivatives (1-16), characterized by H NMR, C NMR and HREI-MS and screened for thymidine phosphorylase inhibitory potential. All derivatives display varied degree of thymidine phosphorylase inhibition in the range of 1.10 ± 0.05 to 49.60 ± 1.30 μM when compared with the standard inhibitor 7-Deazaxanthine having an IC value 38.68 ± 1.12 μM. Structure activity relationships (SAR) has been established for all compounds to explore the role of substitution and nature of functional group attached to the phenyl ring which applies imperious effect on thymidine phosphorylase activity. Molecular docking study was performed to understand the binding interaction of the most active derivatives with enzyme active site.
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| http://dx.doi.org/10.1016/j.bioorg.2018.02.020 | DOI Listing |
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