title: Synthesis and structure-activity relationships of novel compounds for the inhibition of TNF-alpha production.
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.
authors.affiliation: R&D Center, Daewoong Pharm. Co. Ltd., Kyunggi-do, Korea. joonchem@hanmail.net
authors.forename: J S
authors.initials: JS
authors.lastname: Park
authors.forename: K U
authors.initials: KU
authors.lastname: Balk
authors.forename: H J
authors.initials: HJ
authors.lastname: Son
authors.forename: J H
authors.initials: JH
authors.lastname: Lee
authors.forename: S J
authors.initials: SJ
authors.lastname: Lee
authors.forename: J Y
authors.initials: JY
authors.lastname: Cho
authors.forename: J
authors.initials: J
authors.lastname: Park
authors.forename: E S
authors.initials: ES
authors.lastname: Yoo
authors.forename: Y S
authors.initials: YS
authors.lastname: Byun
authors.forename: M H
authors.initials: MH
authors.lastname: Park
mesh_terms: 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
chemical_list: D010726:Phosphodiesterase Inhibitors; D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide; D020889:Rolipram