Synthesis and SAR studies for the inhibition of TNF-α production. Part 2. 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives

Joon Seok Park; Seong Cheol Moon; Kyung Up Baik; Jae Youl Cho; Eun Sook Yoo; Young Seok Byun; Myung Hwan Park

doi:10.1007/bf02976553

Synthesis and SAR studies for the inhibition of TNF-α production. Part 2. 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives

Joon Seok Park
, Seong Cheol Moon
, Kyung Up Baik
, Jae Youl Cho
, Eun Sook Yoo
, Young Seok Byun
, Myung Hwan Park

Daewoong Pharmaceutical Co., Ltd.

Research output: Contribution to journal › Article › peer-review

22 Scopus citations

Abstract

This study describes the synthesis and in vitro evaluation of 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of TNF-α production. From this study, we have found the 6-C position on isoindolinone ring is an optimal derivatization site. Among the compounds synthesized, 6-amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (6) was the most potent in inhibitory activity of TNF-α production in LPS-stimulated RAW264.7 cells.

Original language	English
Pages (from-to)	137-142
Number of pages	6
Journal	Archives of Pharmacal Research
Volume	25
Issue number	2
DOIs	https://doi.org/10.1007/bf02976553
State	Published - Apr 2002
Externally published	Yes

Keywords

6-Amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone
RAW264.7
Structure-activity relationships
TNFα production inhibitor

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10.1007/bf02976553

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title = "Synthesis and SAR studies for the inhibition of TNF-α production. Part 2. 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives",

abstract = "This study describes the synthesis and in vitro evaluation of 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of TNF-α production. From this study, we have found the 6-C position on isoindolinone ring is an optimal derivatization site. Among the compounds synthesized, 6-amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (6) was the most potent in inhibitory activity of TNF-α production in LPS-stimulated RAW264.7 cells.",

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year = "2002",

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doi = "10.1007/bf02976553",

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AU - Baik, Kyung Up

AU - Cho, Jae Youl

AU - Yoo, Eun Sook

AU - Byun, Young Seok

AU - Park, Myung Hwan

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Synthesis and SAR studies for the inhibition of TNF-α production. Part 2. 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives

Abstract

Keywords

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