227094-97-5

Upstream product

• 87-66-1 2-hydroxyresorcinol 
• 140-53-4 p-chlorobenzyl cyanide 
• 1878-66-6 4-chlorophenylacetic Acid 

Downstream Products

• 227094-98-6 3-(4-chlorophenyl)-7,8-dihydroxy-4H-chromen-4-one 
• 227095-04-7 3-(4-chloro-phenyl)-7,8-dihydroxy-2-trifluoromethyl-chromen-4-one 
• 1224164-24-2 4-(2-(4-chlorophenyl)-1-(4-hydroxyphenylimino)ethyl)benzene-1,2,3-triol 
• 1224164-20-8 4-(2-(4-chlorophenyl)-1-(p-tolylimino)ethyl)benzene-1,2,3-triol 
• 1224164-22-0 4-(2-(4-chlorophenyl)-1-(4-chlorophenylimino)ethyl)benzene-1,2,3-triol 
• 1224164-23-1 4-(2-(4-chlorophenyl)-1-(4-nitrophenylimino)ethyl)benzene-1,2,3-triol 
• 1224164-21-9 4-(1-(4-bromophenylimino)-2-(4-chlorophenyl)ethyl)benzene-1,2,3-triol 
• 1219800-81-3 4-(4-chlorophenethyl)phen-1,2,3-triol 
• 1241384-52-0 2-(4-chlorophenyl)-1-(2,3-dihydroxy-4-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)phenyl)ethanone 
• 227095-02-5 3-(4-chloro-phenyl)-7,8-dihydroxy-2-methyl-chromen-4-one 
• 227095-00-3 acetic acid 7-acetoxy-3-(4-chloro-phenyl)-2-methyl-4-oxo-4H-chromen-8-yl ester 

Relevant academic research and scientific papers

Discovery and Development of Small-Molecule Inhibitors of Glycogen Synthase

The overaccumulation of glycogen appears as a hallmark in various glycogen storage diseases (GSDs), including Pompe, Cori, Andersen, and Lafora disease. Accumulating evidence suggests that suppression of glycogen accumulation represents a potential therapeutic approach for treating these GSDs. Using a fluorescence polarization assay designed to screen for inhibitors of the key glycogen synthetic enzyme, glycogen synthase (GS), we identified a substituted imidazole, (rac)-2-methoxy-4-(1-(2-(1-methylpyrrolidin-2-yl)ethyl)-4-phenyl-1H-imidazol-5-yl)phenol (H23), as a first-in-class inhibitor for yeast GS 2 (yGsy2p). Data from X-ray crystallography at 2.85 ?, as well as kinetic data, revealed that H23 bound within the uridine diphosphate glucose binding pocket of yGsy2p. The high conservation of residues between human and yeast GS in direct contact with H23 informed the development of around 500 H23 analogs. These analogs produced a structure-activity relationship profile that led to the identification of a substituted pyrazole, 4-(4-(4-hydroxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)pyrogallol, with a 300-fold improved potency against human GS. These substituted pyrazoles possess a promising scaffold for drug development efforts targeting GS activity in GSDs associated with excess glycogen accumulation.

Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors

Phosphatidylinositol 3-kinase α (PI3Kα) is one of the most attractive therapeutic targets for cancer treatment. As our continuing endeavor to discover isoform and/or mutant selective class of PI3K inhibitors, herein we report the optimization of a structu

Design and synthesis of novel deoxybenzoin derivatives as FabH inhibitors and anti-inflammatory agents

β-Ketoacyl-acyl carrier protein synthase III (FabH) catalyzes the initial step of fatty acid biosynthesis via a type II fatty acid synthase in most bacteria. The important role of this essential enzyme combined with its unique structural features and ubiq

The synthesis, structure and activity evaluation of pyrogallol and catechol derivatives as Helicobacter pylori urease inhibitors

Some pyrogallol and catechol derivatives were synthesized, and their urease inhibitory activity was evaluated by using acetohydroxamic acid (AHA), a well known Helicobacter pylori urease inhibitor, as positive control. The assay results indicate that many compounds have showed potential inhibitory activity against H. pylori urease. 4-(4-Hydroxyphenethyl)phen-1,2-diol (2a) was found to be the most potent urease inhibitor with IC50s of 1.5 ± 0.2 μM for extracted fraction and 4.2 ± 0.3 μM for intact cell, at least 10 times and 20 times lower than those of AHA (IC50 of 17.2 ± 0.9 μM, 100.6 ± 13 μM), respectively. This finding indicate that 2a would be a potential urease inhibitor deserves further research. Molecular dockings of 2a into H. pylori urease active site were performed for understanding the good activity observed.

Metronidazole-deoxybenzoin derivatives as anti-Helicobacter pylori agents with potent inhibitory activity against HPE-induced interleukin-8

A series of new metronidazole-deoxybenzoin derivatives were synthesized and evaluated for their antimicrobial activity against Helicobacter pylori. Highly selective anti-H. pylori activity was also observed in synthesized compounds. Compound 34 exhibited

Discovery of novel 2′,3′,4′-trihydroxy-2- phenylacetophenone derivatives as anti-gram-positive antibacterial agents

A number of 2′,3′,4′-trihydroxy-2-phenylacetophenone derivatives were synthesized and examined for growth inhibition of several kinds of bacteria. 2′,3′,4′-Trihydroxy-2-phenylacetophenone itself exhibited no antibacterial activity, but some of its derivat

Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2

Human lipoxygenase (hLO) isozymes have been implicated in a number of disease states and have attracted much attention with respect to their inhibition. One class of inhibitors, the flavonoids, have been shown to be potent lipoxygenase inhibitors but their study has been restricted to those compounds found in nature, which have limited structural variability. We have therefore carried out a comprehensive study to determine the structural requirements for flavonoid potency and selectivity against platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2. We conclude from this study that catechols are essential for high potency, that isoflavones and isoflavanones tend to select against 12-hLO, that isoflavans tend to select against 15-hLO-1, but few flavonoids target 15-hLO-2.

Synthetic analogs of xanthocercin

Synthetic analogs of xanthocercin in the molecules of which benzodioxole, benzodioxane, or benzodioxepane fragments are annellated to a γ-pyrone ring have been obtained. The structures of the new compounds have been confirmed by analytical and spectral re