Synthesis and structure-activity relationships of novel compounds for the inhibition of TNF-α production

被引:0
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作者
Joon Seok Park
Kyong Up Baik
Ho Jung Son
Jae Ho Lee
Se Jong Lee
Jae Youl Cho
Jisoo Park
Eun Sook Yoo
Young Seok Byun
Myung Hwan Park
机构
[1] R&D Center,
[2] Daewoong Pharm. Co. Ltd.,undefined
来源
关键词
2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone; TNF-α production inhibitor; PDE 4 inhibition; Structure-activity relationship;
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摘要
This study describes the synthesis,in vitro evaluation and molecular modeling study of novel compounds for the inhibition of TNF-α production. Among these compounds, 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (9) was selected as a lead compound and its pyridine derivative10 was more potent in activity and safer than rolipram.
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页码:332 / 337
页数:5
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