Synthesis and bioactivities of novel pyridazine derivatives: inhibitors of interleukin-1 beta (IL-1beta) production.
New pyridazine derivatives were prepared, and their abilities to inhibit IL-1beta production were evaluated. Some compounds showed potent inhibitory activity against IL-1beta production in HL-60 cells stimulated with lipopolysaccharide (LPS). The synthesis and structure-activity relationships of these compounds are described.
Matsuda
T
T
Tokyo Research Laboratories, Kowa Company Ltd., 2-17-43, Noguchi-Cho, Higashimurayama, Tokyo 189-0022, Japan. tamatuda@kowa.co.jp
Aoki
T
T
Ohgiya
T
T
Koshi
T
T
Ohkuchi
M
M
Shigyo
H
H
D000818:Animals; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D018922:HL-60 Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D007375:Interleukin-1 / Q000037:antagonists & inhibitors*; D008070:Lipopolysaccharides; D051379:Mice; D011724:Pyridazines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D005466:Fluorocarbons
D007375:Interleukin-1; D008070:Lipopolysaccharides; D011724:Pyridazines; C442393:6-(2,3,4,5,6-pentafluorophenoxy)-3,4-bis(4-methoxyphenyl)pyridazine; D005466:Fluorocarbons