期刊
PHARMACEUTICALS
卷 15, 期 3, 页码 -出版社
MDPI
DOI: 10.3390/ph15030282
关键词
docking; non-steroidal anti-inflammatory drugs; drug discovery; lipoxygenase; cyclooxygenase
资金
- Deanship of Scientific Research, Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Saudi Arabia [GRANT225]
This study discovered two novel benzimidazole piperidine and phenoxy pyridine derivatives that achieve anti-inflammatory effects through selective inhibition of COX-2, and they have favorable safety profiles.
The goal of achieving anti-inflammatory efficacy with the fewest possible adverse effects through selective COX-2 inhibition is still being investigated in order to develop drugs with safe profiles. This work shows the efficacy and safety profile of two novel benzimidazole piperidine and phenoxy pyridine derivatives in reaching this goal, which would be considered a major achievement in inflammatory therapy. The compounds were evaluated by virtual screening campaign, in vitro cyclooxygenase 1 and 2 (COX-1 and COX-2) inhibition, in vivo carrageenan-induced rat paw edema assay, cytotoxicity against Raw264.7 cells, and histopathological examination of rat paw and stomach. Two new compounds, compound 1 ([(2-{[3-(4-methyl-1H-benzimidazol-2-yl)piperidin-1-yl]carbonyl}phenyl)aminolacetic acid) and compound 2 (ethyl 1-(5-cyano-2-hydroxyphenyl)-4-oxo5-phenoxy-1,4-dihydropyridine-3-carboxylate) showed high selectivity against COX-2, favourable drug-likeness and ADME descriptors, a lack of cytotoxicity, relived paw edema, and inflammation without noticeable side effects on the stomach. These two compounds are promising new NSAIDs.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据