42833-84-1Relevant academic research and scientific papers
Synthetic flavonoid derivatives targeting the glycogen phosphorylase inhibitor site: QM/MM-PBSA motivated synthesis of substituted 5,7-dihydroxyflavones, crystallography, in vitro kinetics and ex-vivo cellular experiments reveal novel potent inhibitors
Chetter, Ben A.,Kyriakis, Efthimios,Barr, Daniel,Karra, Aikaterini G.,Katsidou, Elisabeth,Koulas, Symeon M.,Skamnaki, Vassiliki T.,Snape, Timothy J.,Psarra, Anna-Maria G.,Leonidas, Demetres D.,Hayes, Joseph M.
, (2020/08/10)
Glycogen phosphorylase (GP) is an important target for the development of new anti-hyperglycaemic agents. Flavonoids are novel inhibitors of GP, but their mode of action is unspecific in terms of the GP binding sites involved. Towards design of synthetic
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness
Stefanachi, Angela,Mangiatordi, Giuseppe Felice,Tardia, Piero,Alberga, Domenico,Leonetti, Francesco,Niso, Mauro,Colabufo, Nicola Antonio,Adamo, Carlo,Nicolotti, Orazio,Cellamare, Saverio
, p. 820 - 831 (2016/11/11)
In a recent investigation carried out on a panel of trimethoxybenzanilides, we showed that the formation of an intramolecular hydrogen bond is a key element for tuning P-gp inhibitory activity. In this study, we designed new structurally simplified trimet
Synthesis and antibacterial activity of 4,6-dimethoxy-2-(4-methoxyphenyl)benzofuran-3-yl-methanone derivatives and its intermediates
Krishna Reddy,Venkateswara Rao,Bhaskar Reddy,Ram,Balram
, p. 2245 - 2248 (2015/12/01)
Encouraged by the interesting biological activities associated with benzo[b]furan derivatives, we report here the synthesis, spectroscopic identification and antibacterial activity of benzo[b]furan derivatives (6a-6g) prepared from commercially available,
Trimethoxybenzanilide-based P-glycoprotein modulators: An interesting case of lipophilicity tuning by intramolecular hydrogen bonding
Tardia, Piero,Stefanachi, Angela,Niso, Mauro,Stolfa, Diana Antonella,Mangiatordi, Giuseppe Felice,Alberga, Domenico,Nicolotti, Orazio,Lattanzi, Gianluca,Carotti, Angelo,Leonetti, Francesco,Perrone, Roberto,Berardi, Francesco,Azzariti, Amalia,Colabufo, Nicola Antonio,Cellamare, Saverio
, p. 6403 - 6418 (2014/10/16)
One of the principal reasons for the chemotherapy failure is the overexpression of drug efflux pumps, ABCB1 (also known as MDR1 or P-gp) and ABCC1 (also known as MRP1), whose inhibition remains a priority to circumvent drug resistance. We have recently sh
Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth
Thévenin, Marion,Thoret, Sylviane,Grellier, Philippe,Dubois, Jo?lle
supporting information, p. 4885 - 4892 (2013/09/02)
A series of polysubstituted benzofuran derivatives was easily and rapidly prepared using a tandem Sonogashira coupling/cyclization reaction. Subsequent acylation afforded a small library of 39 new compounds that were assayed in cellulo on Plasmodium falci
Metal-free aryltrifluoromethylation of activated alkenes
Kong, Wangqing,Casimiro, Maria,Fuentes, Noelia,Merino, Estibaliz,Nevado, Cristina
supporting information, p. 13086 - 13090 (2014/01/06)
Metal-free: The first metal-free aryltrifluoromethylation of activated alkenes has been developed. With this method, trifluoromethylated isoquinolinediones, spirobicycles, oxindoles, and α-aryl-β- trifluoromethylamides were obtained with high control of the regioselectivity. Copyright
2'-Substituted chalcone derivatives as inhibitors of interleukin-1 biosynthesis
Batt,Goodman,Jones,Kerr,Mantegna,McAllister,Newton,Nurnberg,Welch,Covington
, p. 1434 - 1442 (2007/10/02)
A series of 2'-substituted chalcone derivatives has been found to show potent inhibition of the production of IL-1β from human peripheral blood monocytes stimulated with lipopolysaccharide (LPS), with IC50 values in the 0.2-5.0-μM range. Some members of the series have also shown inhibition of septic shock induced in mice by injection of LPS, although with low potency. Qualitative structure-activity relationships have shown that the enone is required for activity, which may be mediated by conjugate addition of a biological nucleophile to the chalcone. Electron-poor aromatic rings β to the ketone give enhanced potency. Although electronic effects in the other ring (directly attached to the ketone) are minimal, this ring must possess an ortho substituent for good activity without cytotoxicity, suggesting a degree of selectivity which would not be expected for simple, nonspecific alkylating agents.
Benzamides, compositions and agricultural method
-
, (2008/06/13)
N-Aryl benzamides wherein the aryl group is a nitrogen containing heterocycle are useful as selective herbicidal agents. Compositions containing the novel benzamides and a herbicidal method of selective weed control are disclosed.
