Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents
2020; Elsevier BV; Volume: 30; Issue: 13 Linguagem: Inglês
10.1016/j.bmcl.2020.127237
ISSN1464-3405
AutoresXian-Jing Zheng, Chunshi Li, Mingyue Cui, Ze-Wen Song, Xueqian Bai, Chengwu Liang, Huiyan Wang, Tianyi Zhang,
Tópico(s)Synthesis and Biological Evaluation
ResumoTwenty 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 8l 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+ 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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