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 more potent in activity and safer than rolipram.
Park
J S
JS
R&D Center, Daewoong Pharm. Co. Ltd., Kyunggi-do, Korea. joonchem@hanmail.net
Balk
K U
KU
Son
H J
HJ
Lee
J H
JH
Lee
S J
SJ
Cho
J Y
JY
Park
J
J
Yoo
E S
ES
Byun
Y S
YS
Park
M H
MH
D000818:Animals; D051379:Mice; D008954:Models, Biological; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology; D020889:Rolipram / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013792:Thalidomide / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors* / Q000096:biosynthesis
D010726:Phosphodiesterase Inhibitors; D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide; D020889:Rolipram