134271-76-4Relevant articles and documents
Application of natural phosphate modified with sodium nitrate in the synthesis of chalcones: A soft and clean method
Sebti, Said,Solhy, Abderrahim,Tahir, Rachid,Abdelatif, Smahi,Boulaajaj, Said,Mayoral, Jose A.,Garcia, Jose I.,Fraile, Jose M.,Kossir, Abdelali,Oumimoun, Hammou
, p. 1 - 6 (2003)
The solid obtained by impregnation of natural phosphate (NP) with a solution of sodium nitrate, followed by calcination at 900°C, is a strongly basic catalyst that is easily prepared from cheap precursors. The catalytic activity of this solid in the Claisen-Schmidt condensation was studied and high yields were obtained with small amounts of catalyst. The reaction rate depends on the substitution in both benzaldehyde and acetophenone derivatives. The effect of the solvent, as well as the addition of water and ammonium salt, was investigated as well. The catalyst can be easily recovered and efficiently reused.
Synthesis and biological activity of new chalcone scaffolds as prospective antimicrobial agents
Narwal, Sangeeta,Kumar, Sanjiv,Verma, Prabhakar Kumar
, p. 1625 - 1641 (2021/01/20)
Chalcones are open-chain flavonoids which contains two aromatic rings are joined by 3-carbons α-, β-unsaturated carbonyl chain. The, β-unsaturated ketonic group which is liable for the antimicrobial activity of the chalcone is additionally of vast use in
Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors
Jain, Priti,Wadhwa, Pankaj K.,Rohilla, Shilpa,Jadhav, Hemant R.
supporting information, p. 33 - 37 (2015/12/18)
BACE-1 (β-secretase) is considered to be one of the promising targets for treatment of Alzheimer's disease as it catalyzes the rate limiting step of Aβ-42 production. Herein, we report a novel class of allylidene hydrazinecarboximidamide derivatives as moderately potent BACE-1 inhibitors, having aminoguanidine substitution on allyl linker with two aromatic groups on either side. A library of derivatives was designed based on the docking studies, synthesized and evaluated for BACE-1 inhibition in vitro. The designed ligands displayed interactions with the catalytic aspartate dyad through guanidinium functionality. Further, the aromatic rings placed on either side of the linker occupied S1 and S3 active site regions contributing to the activity. These ligands were also predicted to follow Lipinski rule and cross blood brain barrier. Compound 2.21, having high docking score, was found to be most active with IC50 of 6.423 μM indicating good correlation with docking prediction.
Effects of structural and electronic characteristics of chalcones on the activation of peroxisome proliferator-activated receptor gamma
Schott, Jason Taylor,Mordaunt, Charles Edward,Vargas, Anthony Joseph,Leon, Martin Antonio,Chen, Kevin Hsinwen,Singh, Mandeep,Satoh, Mikiko,Cardenas, Emilio Leal,Maitra, Santanu,Patel, Nilay Vinod,De Lijser, Hubrecht Johan Peter
, p. 229 - 236 (2013/03/14)
Chalcones share some structural similarities with GW-1929, a highly-selective and potent agonist for peroxisome proliferator-activated receptor-gamma (PPARγ). In this study, we tested 53 structurally diverse chalcones to identify characteristics essential for PPARγ activation in a GAL4-based transactivation assay. This screen identified several novel chalcone agonists of PPARγ. Our results indicate that chalcones with an electron rich group or sterically large groups such as naphthyl on the carbonyl side tend to activate PPARγ. The absence of any strict structural or electronic requirements suggests that the flexibility of the PPARγ ligand binding pocket may allow binding of diverse chalcones with some preference for a slightly larger electron-rich group on the carbonyl side. We predict that further structure-activity relationship studies on chalcones with naphthalene or electron-rich groups near the carbonyl moiety will lead to the development of more potent PPARγ agonists.
