301358-84-9Relevant academic research and scientific papers
A substituted 3,4-dihydropyrimidinone derivative (compound D22) prevents inflammation mediated neurotoxicity; Role in microglial activation in BV-2 cells
Kwon, Oh Wook,Moon, Eunjung,Chari, Murugulla A.,Kim, Tae Woo,Kim, Ae-Jung,Lee, Pyeongjae,Ahn, Kwang-Hyun,Kim, Sun Yeou
, p. 5199 - 5203 (2012)
A novel synthetic 3,4-dihydropyrimidinone derivative, compound D22 (ethyl 6-methyl-4-(3-phenoxyphenyl)-2-thioxo-3,4-dihydropyrimidine-5-carboxylate), was found to exert anti-inflammatory properties in lipopolysaccharide-stimulated microglial BV-2 cells. Compound D22 reduced the pro-inflammatory factors such as nitric oxide, prostaglandin E2, tumor necrosis factor-α and interleukin-1β. Moreover, it suppressed the expressions of inducible NO synthase and cyclooxygenase-2. Compound D22 inhibited the activation of mitogen-activated protein kinases. When compound D22-conditioned media from BV-2 cells were applied to N2a cells, neuronal cell death was inhibited via suppression of caspase-3 activation and regulation of Bcl-2 and Bax proteins expression. These results suggest that compound D22 may be useful for treating neurodegenerative diseases related with neuroinflammation.
Synthesis of 3,4-dihydropyrimidin-2-ones (DHPMs) using mesoporous aluminosilicate (AlKIT-5) catalyst with cage type pore structure
Shobha,Chari,Mano,Selvan,Mukkanti,Vinu
experimental part, p. 10608 - 10611 (2010/02/27)
Here we demonstrate on the synthesis of 3,4-dihydropyrimidin-2-ones (DHPMs) and their derivatives through a three-component condensation reactions of aldehyde, β-ketoester and urea or thiourea using mesoporous aluminosilicate (AlKIT-5) nanocage as catalyst and acetonitrile as solvent under reflux conditions. The catalyst was found to be highly active and selective, affording a high yield of DHPMs. Compared to the classical Biginelli reaction conditions, this new approach consistently has the advantage of excellent yields (80-96%) and short reaction times, 3.0-4.0 h. The effect of the acidity and the concentration of the catalyst on the above process was investigated. We also demonstrate the synthesis of various multifunctional Biginelli compounds using the highly active AlKIT-5 catalysts.
