21962-50-5

Upstream product

• 34841-06-0 3-bromo-4-methoxybenzylaldehyde 
• 544-92-3 copper(I) cyanide 
• 4367-08-2 copper(II) cyanide 
• 2973-78-6 3-bromo-4-hydroxybenzylaldehyde 
• 35450-37-4 methyl 3-bromo-4-methoxybenzoate 
• 121-98-2 methyl 4-methoxybenzoate 
• 25978-74-9 3-Cyano-4-methoxy-benzoic acid methyl ester 
• 310424-35-2 5-hydroxymethyl-2-methoxy-benzonitrile 
• 69455-12-5 4-benzyloxy-3-bromobenzaldehyde 
• 73289-79-9 5-formyl-2-hydroxybenzonitrile 
• 77-78-1 dimethyl sulfate 
• 123-08-0 4-hydroxy-benzaldehyde 
• 74-88-4 methyl iodide 

Downstream Products

• 125872-38-0 3-carbamoyl-4-methoxy-benzaldehyde 
• 934470-20-9 3-cyano-N-hydroxy-4-methoxybenzenecarboximidoyl chloride 
• 934470-22-1 ethyl 3-(3-cyano-4-hydroxyphenyl)-5-isoxazolecarboxylate 
• 934470-21-0 ethyl 3-(3-cyano-4-methoxyphenyl)-5-isoxazolecarboxylate 
• 934470-19-6 5-[(hydroxyimino)methyl]-2-methoxybenzonitrile 
• 269411-78-1 2-benzyloxy-5-formyl-benzamide 
• 76143-20-9 5-formyl-2-hydroxy-benzamide 
• 310464-95-0 N-(2'-tert-butylsulfamoyl-biphenyl-4-yl)-3-(3-cyano-4-methoxy-phenyl)-acrylamide 
• 310464-94-9 (Z)-3-(3-Cyano-4-methoxy-phenyl)-acrylic acid methyl ester 

Relevant academic research and scientific papers

3-(5-METHOXY-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of formula (I') and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.

Water-soluble 4-hydroxystyryl and 4-hydroxyphenyl-butadienyls dyes with switchable fluorescence

Fluorescent 4-hydroxystyryl dyes are useful for many biomedical and pharmaceutical assays, and other analyte sensing applications. However, these dyes often suffer from limited applicability in analytical and bioanalytical utilization due to insufficient water-solubility, high acid-ionization constants (pKa) and short-wavelength absorption and emission. To solve these issues, a series of new, water-soluble 4-hydroxystyryl and longer-wavelength 4-hydroxyphenyl-butadienyl dyes were synthesized and the spectral and protolytic properties were studied. These new dyes contain electron-withdrawing substituents ortho to the triggering 4-hydroxyl group. The introduction of the cyano and formyl groups was found to decrease the pKa and extend the pH-sensing region of these fluorophores. In respect of the molecular structure, these dyes exhibit either a “turn-on” activatable fluorescence, or a dual-fluorescence that enables ratiometric measurements. The 4-hydroxyphenyl-butadienyl dye was evaluated for fluorescence monitoring of drug delivery. These new dyes are promising fluorophores for acidity measurements and other sensing applications.

Design, synthesis and biological evaluation of 1-hydroxy-2-phenyl-4-pyridyl-1H-imidazole derivatives as xanthine oxidase inhibitors

In our previous study, we reported a series of 1-hydroxy-2-phenyl-1H-imidazole-5-carboxylic acid derivatives that presented excellent in vitro xanthine oxidase inhibitory potency. As a continuation study, a series of 1-hydroxy-2-phenyl-1H-imidazole derivatives containing a pyridine moiety (4a-g and 5a-g) at the 4-position was designed and synthesized. Evaluation of in vitro xanthine oxidase inhibition demonstrated that the 4a-g series was more potent than the 5a-g series. Compound 4f was the most promising derivative in the series with an IC50 value of 0.64 μM. A Lineweaver-Burk plot revealed that compound 4f acted as a mixed-type xanthine oxidase inhibitor. An iso-pentyloxy group at the 4′-position improved the inhibitory potency. More interestingly, structure-activity relationship analysis indicated that the pyridine para-N atom played a crucial role in the inhibition. Molecular modeling provided a reasonable explanation for the structure-activity relationships observed in this study. In addition, a three dimensional quantitative structure-activity relationships model which possessed reasonable statistics (q2 = 0.885 and r2 = 0.993) was conducted to further understand the structural basis of these compounds as xanthine oxidase inhibitors. These compounds, especially compound 4f, have good potential for further investigations.

HETEROCYCLIC-IMIDAZOLE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a heterocyclic-imidazole derivative, a preparation method therefor, and a medical use thereof, and particularly to a new heterocyclic-imidazole derivative of general Formula (I), a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof as a therapeutic agent, particularly as a poly(ADP-ribose)polymerase (PARP) inhibitor.

Heterocycle and imidazole compounds, pharmaceutical composition comprising heterocycle and imidazole derivatives as well as preparation method and application of heterocycle and imidazole compounds

The invention relates to heterocycle and imidazole derivatives as well as a preparation method and a pharmaceutical application of heterocycle and imidazole derivatives, in particular to novel heterocycle and imidazole derivatives as shown in the general formula (I), a preparation method of the heterocycle and imidazole derivatives, pharmaceutical composition comprising the heterocycle and imidazole derivatives as well as an application of the heterocycle and imidazole derivatives as a therapeutic agent and particularly as a PARP (poly (ADP-ribose) polymerase) inhibitor.

Synthesis and evaluation of 1-hydroxy/methoxy-4-methyl-2-phenyl-1 H-imidazole-5-carboxylic acid derivatives as non-purine xanthine oxidase inhibitors

Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid, whose overproduction leads to the gout-causing hyperuricemia. In this study, a series of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives (4ae4k and 6ae6k) was synthesized and evaluated for their inhibitory potency against xanthine oxidase. The 1-hydroxyl substituted derivatives 4ae4k showed excellent inhibitory potency with IC50 values ranging from 0.003 μM to 1.2 μM, with compounds 4d (IC50= 0.003 μM), 4e (IC50 = 0.003 μM), and 4f (IC50 = 0.006 μM) manifesting the most potent xanthine oxidase inhibitory potency that were comparable with that of Febuxostat (IC50 = 0.01 μM). LineweavereBurk plot analysis revealed that representative compound 4f acted as a mixed-type inhibitor for xanthine oxidase. The basis of significant inhibition of xanthine oxidase by 4f was rationalized by its molecular docking into the active site of xanthine dehydrogenase.

Substituted benzamide inhibitors of rhinovirus 3C protease

Nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease are described.

Substituted benzamide inhibitors of human rhinovirus 3C protease: Structure-based design, synthesis, and biological evaluation

A series of nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease was identified using structure-based design. The design, synthesis, and biological evaluation of these inhibitors are reported. A Michael acceptor was combined with a benzamide core mimicking the P1 recognition element of the natural 3CP substrate, α,β-Unsaturated cinnamate esters irreversibly inhibited the 3CP and displayed antiviral activity (EC50 0.60/μM, HRV-16 infected H1-HeLa cells). On the basis of cocrystal structure information, a library of substituted benzamide derivatives was prepared using parallel synthesis on solid support. A 1.9 A? cocrystal structure of a benzamide inhibitor in complex with the 3CP revealed a binding mode similar to that initially modeled wherein covalent attachment of the nucleophilic cysteine residue is observed. Unsaturated ketones displayed potent reversible inhibition but were inactive in the cellular antiviral assay and were found to react with nucleophilic thiols such as DTT.