Abstract
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.
MeSH terms
-
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
Substances
-
Phosphodiesterase Inhibitors
-
Tumor Necrosis Factor-alpha
-
Thalidomide
-
Rolipram