70768-92-2Relevant academic research and scientific papers
Mono- and di-substituted 5,6-diphenyl-3-alkylaminopyridazines active as ACAT inhibitors
Toma, Lucio,Giovannoni, Maria Paola,Dal Piaz, Vittorio,Kwon, Byoung-Mog,Kim, Young-Kook,Gelain, Arianna,Barlocco, Daniela
, p. 39 - 46 (2007/10/03)
A series of mono- or di-para-substituted 5,6-diphenyl-3-alkylaminopyridazines were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. The compound which combines a chlorine atom on the 6-phenyl ring and a n-hexylamino chain showed a significant enhancement of activity with respect to the unsubstituted derivative. Attempts to correlate the activity of the compounds to their structural features, also through theoretical calculations, are reported.
Pyridazine compounds and compositions containing the same
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Page column 15, (2008/06/13)
This invention relates to pyridazine derivatives represented by the formula (1): wherein R1represents a (substituted) aryl group, R2represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.
Synthesis and bioactivities of novel 5,6-Bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives: Inhibitors of interleukin-1 beta (IL-1β) production
Matsuda, Takayuki,Aoki, Taro,Koshi, Tomoyuki,Ohkuchi, Masao,Shigyo, Hiromichi
, p. 2373 - 2375 (2007/10/03)
New 5,6-bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives were prepared, and their abilities to inhibit IL-1β production were evaluated. Some compounds showed potent inhibitory activity against IL-1β production in HL-60 cells stimulated with lipopolysaccharide (LPS). The synthesis and structure-activity relationships of these compounds are described.
