Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 13, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127237
Keywords
Benzothiazole; 1,3,4-Oxadiazole; Anti-oxidant activity; Anti-inflammatory activity; COX-2 inhibition
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Funding
- Department of Education of Jilin Province [JJKH20191070KJ]
- Health Department of Jilin Province [2018ZC034]
- Doctoral Foundation of Jilin Medical University [JYBS2018007]
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Twenty benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety were synthesized and evaluated for their anti-oxidant and anti-inflammatory activities. Among these compounds, 8h and 81 were appeared to have high radical scavenging efficacies as 0.05 +/- 0.02 and 0.07 +/- 0.03 mmol/L of IC50, values in ABTS(+center dot) bioassay, respectively. In anti-inflammatory tests, compound 8h displayed good activity with 57.35% inhibition after intraperitoneal administration, which was more potent than the reference drug (indomethacin). Molecular modeling studies were performed to investigate the binding mode of the representative compound 8h into COX-2 enzyme. In vitro enzyme study implied that compound 8h exerted its anti-inflammatory activity through COX-2 inhibition.
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