Synthesis and bioactivities of novel 5,6-bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives: inhibitors of interleukin-1 beta (IL-1beta) production.
New 5,6-bis(4-methoxyphenyl)-2H-pyridazin-3-one 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
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T
Tokyo Research Laboratories, Kowa Company Ltd., 2-17-43, Noguchi-Cho, Higashimurayama, Tokyo 189-0022, Japan. tamatuda@kowa.co.jp
Aoki
T
T
Koshi
T
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Ohkuchi
M
M
Shigyo
H
H
D000284:Administration, Oral; D000818:Animals; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D018922:HL-60 Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007375:Interleukin-1 / Q000037:antagonists & inhibitors*; D011724:Pyridazines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
C442394:1-(4-chlorocinnamyl)-3,4-bis(4-methoxyphenyl)-1H-pyridazin-6-one; D007375:Interleukin-1; D011724:Pyridazines