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

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 mor...

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Bibliographic Details
Published in:Archives of pharmacal research 2000-08, Vol.23 (4), p.332-337
Main Authors: Park, J S, Balk, K U, Son, H J, Lee, J H, Lee, S J, Cho, J Y, Park, J, Yoo, E S, Byun, Y S, Park, M H
Format: Article
Language:English
Subjects:
Animals
Mice
Models, Biological
Phosphodiesterase Inhibitors - pharmacology
Rolipram - pharmacology
Structure-Activity Relationship
Thalidomide - pharmacology
Tumor Necrosis Factor-alpha - antagonists & inhibitors
Tumor Necrosis Factor-alpha - biosynthesis
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Summary: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.
ISSN:0253-6269
1976-3786
DOI:10.1007/BF02975443