936574-32-2

Upstream product

• 123-08-0 4-hydroxy-benzaldehyde 
• 4257-94-7 β-D-allose pentaacetate 
• 108-24-7 acetic anhydride 
• 80154-34-3 formaldehydephenlyl-O-β-D-pyranosyl alloside 

Downstream Products

• 105054-56-6 4-(hydroxymethyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-allopyranoside 
• 80154-34-3 formaldehydephenlyl-O-β-D-pyranosyl alloside 
• 1234273-62-1 C₂₇H₃₂N₂O₁₂ 
• 1234273-63-2 C₂₇H₃₂N₂O₁₁S 
• 1234273-64-3 C₂₇H₃₂N₂O₁₃ 
• 1234273-65-4 C₂₇H₃₂N₂O₁₂S 
• 1234273-66-5 C₂₈H₃₄N₂O₁₃ 
• 1234273-67-6 C₂₈H₃₄N₂O₁₂S 

Relevant academic research and scientific papers

SLAP reagents for the photocatalytic synthesis of C3/C5-substituted, N-unprotected selenomorpholines and 1,4-selenazepanes

Herein, we disclose the first set of unique selenium-containing SLAP (SiLicon Amine Protocol) reagents for the direct synthesis of C3/C5-substituted selenomorpholines and 1,4-selenazepanes fromdiverse (hetero)aldehydes under mild photocatalytic conditions. Enantiomerically pure 1,2-amino alcohol/α-amino acid versions of these heterocycles were also synthesized. Further, we have shown the late-stage modification of certain biologically active agents using the developed seleno-SLAPreagents.

Synthesis and antitumor activity of a novel series of helicid-pyrrolidone derivatives

This paper reports the synthesis of a new series of helicid-pyrrolidone derivatives (4a-4d, 5a-5d, and 6a-6d), which were tested for antitumor activity against human skov3 cell. In this study, two compounds (4b and 6c) demonstrate high antitumor activity

Preparation method of glucoside and derivatives thereof

The invention discloses a preparation method of glucoside and derivatives thereof. According to the method, all hydroxyl groups on a sugar molecule structure are acetylated, a ligand containing phenolic hydroxyl groups is prepared at the same time, then boron trifluoride-diethyl ether is used as a catalyst, the two substances are condensed to obtain tetraacetylated glucoside, and finally acetyl protecting groups are removed to obtain the required glucoside. The method can selectively catalyze hemiacetal hydroxyl of monosaccharide to react with hydroxyl to obtain glucoside, and the product is single. The method is simple in production operation and low in equipment requirement, can be used for synthesizing glucoside and derivatives thereof with similar structures, is green and environment-friendly, and can be used for large-scale production.

Helicid derivatives and process for their preparation and use

The invention relates to compounds shown in formula (I) in the specification or pharmaceutically acceptable salts, aquo-complexes or solvent compounds thereof, as well as a preparation method and an application thereof. Helicianeoide is used as a raw mate

Helicid analogues for treating depression

The invention discloses helicid analogues for treating depression and relates to helicid derivatives such as 4-hydroxymethyl-beta-D-allopyranoside and 4-carboxylphenyl-beta-D-allopyranoside and their medicinal salts, esters and solvates. The helicid deriv

Identification of a novel glycan processing enzyme with exo-acting β-allosidase activity in the Golgi apparatus using a new platform for the synthesis of fluorescent substrates

The majority of eukaryotic proteins undergo post-translational modifications (PTMs) involving the attachment of complex glycans, predominantly through N-glycosylation and O-glycosylation. PTMs play important roles in virtually all cellular processes, and aberrant regulation of protein glycosylation and glycan processing has been implicated in various diseases. However, glycan processing on proteins in various cellular contexts has not been visualized. We had previously developed a quinone methide cleavage (QMC) platform for enhanced substrate design. This platform was applied here to screen for novel glycan-processing enzymes. We designed and synthesized fluorescent substrates with β-allopyranoside residues using the QMC platform. When applied in cell-based assays, the fluorescent substrates allowed rapid and clear visualization of β-allosidase activity in the Golgi apparatus of human cultured cells. The QMC platform will likely find broad applications in visualizing the activities of glycan processing enzymes in living cells and in studying PTMs.

Synthesis and calming activity of helicid derivatives containing the 3,4-dihydropyrimidin-2(H)-one and 3,4-dihydropyrimidine-2(H)-thione moiety

A series of novel helicid derivatives containing 3,4-dihydropyrimidin-2(1H) -one and 3,4-dihydropyrimidine2(1H)-thione moiety (3a-3f and 4a-4f) were synthesized starting from helicid. The structure of the new compounds were characterized by 1H

Synthesis and evaluation of 5-benzylidene(thio)barbiturate-β-d-glycosides as mushroom tyrosinase inhibitors

A series of 5-benzylidene(thio)barbiturate-β-d-glycosides were designed, synthesized and evaluated as a new class of mushroom tyrosinase inhibitors. The results demonstrated that most of compounds had more potent inhibitory activities than arbutin (IC50 8.4 mmol/L). Compound 12b was found to be the most potent inhibitor with IC50 value of 0.05 mmol/L. SARs analysis suggested that (1) 5-benzylidenethiobarbiturate substructures were efficacious for the inhibitory activity; (2) the lipophilic property of acetylated sugar moiety facilitated the inhibitory potency; (3) the hydroxyl group of 3′-configuration contributed to the increase of inhibitory effects. In addition, the inhibition mechanism study revealed that 5-benzylidene(thio)barbiturate-β-d-glycosides were irreversible inhibitors.

Discovery of 4-functionalized phenyl-O-β-d-glycosides as a new class of mushroom tyrosinase inhibitors

A series of 4-functionalized phenyl-O-β-d-glycosides were designed, synthesized and evaluated as a new class of mushroom tyrosinase inhibitors. The results demonstrated that compounds 6a-13a bearing a thiosemicarbazide moiety exhibited potent activities with IC50 values range from 0.31 to 52.8 μM. Particularly, compound 9a containing acetylated glucose moiety was found to be the most active molecule with an IC50 value of 0.31 μM. SARs analysis suggested that (1) the thiosemicarbazide moiety remarkably contributed to the increase of inhibitory effects on tyrosinase; (2) the configuration and bond type of sugar moiety also played a very important role in determining their inhibitory activities. The inhibition kinetics and inhibition mechanism study revealed that compound 9a was reversible and competitive type inhibitor, whereas compound 13a was reversible and competitive-uncompetitive mixed-II type inhibitor.

Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors

A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC50 values of 0.45 ± 0.02 μM, 0.49 ± 0.02 μM, and 0.20 ± 0.01 μM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.