• Title/Summary/Keyword: 2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone

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Nob1e2-[3-(Cyclopentyloxy)-4-Methoxyphenyl]-1-Isoindolinone Derivatives. PartI: Synthesis and SAR Studies for the Inhibition of TNF-$\alpha$ Production

  • Park, Joon-Seok;Baik, Kyong-Up;Cho, Jae-Youl;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.367-370
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    • 2001
  • This study describes the synthesis and in vitro evaluation of noble 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone Derivatives for the inhibition of TNF-$\alpa$ production. Among these compounds, 2- [3- (Cyclopentyloxy)- 4- methoxyphenyll- 3- methyl -1 - isoindolinone (5) was the most potent in inhibitory activity of TNF-$\alpa$ production in LPS-stimulated RAW264.7 cells.

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Synthesis and SAR Studies for the Inhibition of TNF-$\alpha$ Production. Part 2. 2-[3-(Cyclopenthloxy)4-Methoxyphenyl]-Substituted-1-Isoindolinone Derivatives

  • Park, Joon-Seok;Moon, Seong-Cheol;Baik, Kyung-Up;Cho, Jae-Youl;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.25 no.2
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    • pp.137-142
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    • 2002
  • This study describes the synthesis and in vitro evaluation of 2-[3- (Cyclopenthloxy) 4-Methoxyphenyl] - Substituted-1-Isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of $TNF-{\alpha}$ production. From this study, we have found the 6-C position on isoindolinone ring is an optimal derivatization site. Among the compounds synthesized, 6-ammo-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (6) was the most potent in inhibitory activity of $TNF-{\alpha}$ production in LPS-stimulated RAW264.7 cells.

Synthesis and Structure-Activity Relationships of Novel Compounds for the Inhibition of TNF-$\alpha$ Production

  • Park, Joon-Seok;Baik, Kyong-Up;Son, Ho-Jung;Lee, Jae-Ho;Lee, Se-Jong;Choi, Jae-Youl;Park, Ji-Soo;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.332-337
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    • 2000
  • This study describes the synthesis, in vitro evaluation and molecular modeling study of novel compounds for the inhibition of TNF-$\alpha$production, Among these compounds, 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (9) was selected as a lead compound and its pyridine derivative 10 was more potent in activity and safer than rolipram.

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