110694-59-2Relevant articles and documents
Easy access to evans' oxazolidinones. Stereoselective synthesis and antibacterial activity of a new 2-oxazolidinone derivative
Diaz, Gaspar,De Freitas, Michelle A.A.,Ricci-Silva, Maria E.,Diaz, Marisa A.N.
, p. 7429 - 7439 (2014)
An interesting new approach was developed for the synthesis of Evans' chiral auxiliaries with excellent yields. In turn, another new stereoselective and efficient strategy has also allowed for the preparation of a 2-oxazolidinone derivative in 34% overall yield from the Morita-Baylis-Hillman adduct. The antibacterial activity of this oxazolidinone was tested against Staphylococcus aureus strains isolated from animals with mastitis infections.
Molecular discrimination of N-protected amino acid esters by a self-assembled cylindrical capsule: spectroscopic and computational studies.
Hayashida, Osamu,Sebo, Lubomir,Rebek Jr., Julius
, p. 8291 - 8298 (2002)
A self-assembled, cylindrical capsule was used to bind N-alpha-protected amino acid esters. The reversible encapsulation was studied using NMR spectroscopy in deuterated mesitylene solution and by computer-aided molecular modeling. BOC-L-alanine alkyl est
Low molecular weight MPEG-assisted organic synthesis
Figlus, Marek,Tarruella, Albert C.,Messer, Anastasia,Sollis, Steven L.,Hartley, Richard C.
, p. 4405 - 4407 (2010)
A toolkit of low molecular weight MPEG-supported coupling agents ( MIIDQ, MEDCI), reagents for the Mitsunobu reaction ( MDEAD, MTPP), an alternative to diazomethane, and scavengers can be used in the solution-phase synthesis of amides, esters and ureas and are easily removed after use by solid-phase extraction (MSPE) using normal silica.
Construction and activity evaluation of novel benzodioxane derivatives as dual-target antifungal inhibitors
An, Yunfei,Fan, Haiyan,Han, Jun,Liu, Wenxia,Sun, Bin,Xie, Honglei
, (2021/11/09)
Ergosterol exert the important function in maintaining the fluidity and osmotic pressure of fungal cells, and its key biosynthesis enzymes (Squalene epoxidase, SE; 14 α-demethylase, CYP51) displayed the obvious synergistic effects. Therefore, we expected to discover the novel antifungal compounds with dual-target (SE/CYP51) inhibitory activity. In the progress, we screened the different kinds of potent fragments based on the dual-target (CYP51, SE) features, and the method of fragment-based drug discovery (FBDD) was used to guide the construction of three different series of benzodioxane compounds. Subsequently, their chemical structures were synthesized and evaluated. These compounds displayed the obvious biological activity against the pathogenic fungal strains. Notably, target compounds 10a-2 and 22a-2 possessed the excellent broad-spectrum anti-fungal activity (MIC50, 0.125–2.0 μg/mL) and the activity against drug-resistant strains (MIC50, 0.5–2.0 μg/mL). Preliminary mechanism studies have confirmed that these compounds effectively inhibited the dual-target (SE/CYP51) activity, they could cause fungal rupture and death by blocking the bio-synthetic pathway of ergosterol. Further experiments discovered that compounds 10a-2 and 22a-2 also maintained a certain of anti-fungal effect in vivo. In summary, this study not only provided the new dual-target drug design strategy and method, but also discover the potential antifungal compounds.
SYNTHESIS OF AMINO ACID ESTERS BY PAPAIN
Cantacuzene, D.,Pascal, F.,Guerreiro, C.
, p. 1823 - 1826 (2007/10/02)
A wide range of N-Boc-amino acid esters were synthesized from N-Boc-amino acids and alcohol using papain as catalyst.Suitable biphasic reaction mixtures were found for most amino acids to achieve high yield of ester synthesis.With N-Boc-L-aspartic and glutamic acids only the α carbonyl group esterified, without racemisation.
