53774-96-2Relevant academic research and scientific papers
Iridium-catalyzed chemoselective transfer hydrogenation of α, β-unsaturated ketones to saturated ketones in water
Chen, Jinxun,Chen, Yongsheng,Cui, Xiaofeng,Jiang, Xiaolan,Liu, Qixing,Zhou, Haifeng
supporting information, (2022/01/24)
A chemoselective iridium-catalyzed transfer hydrogenation of α, β-unsaturated ketones was realized in water. The C[dbnd]C double bonds of 2-benzylidene indanones and analogues were hydrogenated exclusively catalyzed by an iridium complex (0.1 mol%) bearin
Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice
?rfi, László,Bagóné Vántus, Viola,Garai, János,Garami, András,Jakus, Péter Balázs,Kéringer, Patrik,Kovács, Dominika,Krekó, Marcell,Lóránd, Tamás,Radnai, Balázs,Rumbus, Zoltán,Vámos, Eszter
, p. 1357 - 1369 (2021/07/22)
Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine playing crucial role in immunity. MIF exerts a unique tautomerase enzymatic activity that has relevance concerning its multiple functions and its small molecule inhibitors have been proven to block its pro-inflammatory effects. Here we demonstrate that some of the E-2-arylmethylene-1-tetralones and their heteroanalogues efficiently bind to MIF’s active site and inhibit MIF tautomeric (enolase, ketolase activity) functions. A small set of the synthesised derivatives, namely compounds (4), (23), (24), (26) and (32), reduced inflammatory macrophage activation. Two of the selected compounds (24) and (26), however, markedly inhibited ROS and nitrite production, NF-κB activation, TNF-α, IL-6 and CCL-2 cytokine expression. Pre-treatment of mice with compound (24) exaggerated the hypothermic response to high dose of bacterial endotoxin. Our experiments suggest that tetralones and their derivatives inhibit MIF’s tautomeric functions and regulate macrophage activation and thermal changes in severe forms of systemic inflammation.
Manganese(I)-Catalyzed α-Alkenylation of Ketones Using Primary Alcohols
Gawali, Suhas Shahaji,Pandia, Biplab Keshari,Gunanathan, Chidambaram
supporting information, p. 3842 - 3847 (2019/05/24)
A simple protocol of manganese catalyzed selective α-alkenylation of ketones using primary alcohols is reported. The reactions proceeded well with a low loading of catalyst (0.3 mol %). The overall transformation operates through O-H bond activation of pr
Reactivity of α-arylidene benzoheteracyclanone dibromides toward azide ion: An effective approach to 3-(α-substituted-benzyl)chromones and -1-thiochromones
Patonay,Dinya,Lévai,Molnár
, p. 2895 - 2907 (2007/10/03)
Treatment of dibromides of 3-arylidenechromanones and -1-thiochromanones with sodium azide resulted in the formation of 3-(α-azidobenzyl)chromones and -1-thiochromones whereas dibromides having no antiperiplanar vicinal hydrogen in the ring such as flavanone, 1-thioflavanone and benzosuberone derivatives afforded only the parent enones by bromine elimination. Evidence supported the intermediacy of 3-(α-bromobenzyl)chromones and -1-thiochromones in this reaction. These postulated intermediates were prepared in an independent way and transformed into azides in high yield.
Heterocycles. Part XVII. Synthesis of New Substituted 2,3,3a,4,5,6-Hexahydrobenzocycloheptapyrazoles and Related Compounds
El-Rayyes, N. R.,Bahtiti, N. H.
, p. 209 - 214 (2007/10/02)
Aryl aldehydes I reacted with 1-benzosuberone to yield the corresponding 2-arylidene-1-benzosuberones II.Condensation of II with hydrazine and its derivatives provided the substituted 2,3,3a,4,5,6-hexahydrobenzocycloheptapyrazoles III-VI respe
Heterocycles. Part X. Synthesis of New Pyrimidine Systems
El-Rayyes, N. R.,Ramadan, H. M.
, p. 589 - 596 (2007/10/02)
Selected aryl aldehydes I were reacted with 1-benzosuberone to give the corresponding 2-arylidene-1-benzosuberone II.Condensation of these chalcones with urea and thiourea revealed the formation of the corresponding substituted pyrimidin-2-ones III, and p
