864528-55-2

Upstream product

• 120-20-7 2-(3,4-dimethoxyphenyl)-ethylamine 
• 6380-23-0 3,4-dimethoxystyrene 
• 40173-90-8 3,4-dimethoxyphenethyl bromide 
• 93-40-3 (3,4-Dimethoxyphenyl)acetic acid 
• 75803-23-5 methanesulphonic acid,2-(3,4-dimethoxyphenyl)ethyl ester 
• 7417-21-2 2-(3,4-dimethoxyphenyl)ethyl alcohol 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 121-33-5 vanillin 
• 75010-39-8 1-(3,4-dimethoxyphenyl)-2-(p-toluenesulfonyloxy)ethane 
• 7786-61-0 3-methoxy-4-hydroxystyrene 

Downstream Products

• 1240425-41-5 1-(3,4-dimethoxyphenethyl)-4-hexyl-1H-1,2,3-triazole 
• 1335128-21-6 4-((4-chlorophenyl)(hydroxyl)methyl)-1-(3,4-dimethoxyphenethyl)-1H-1,2,3-triazole 
• 1376605-93-4 1-(3,4-dimethoxyphenethyl)-4-dodecyl-1H-1,2,3-triazole 

Relevant academic research and scientific papers

Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold

The ecto-5′-nucleotidase CD73 is involved in the production of immunosuppressive adenosine in the tumoral microenvironment and recently became a validated target in immuno-oncology. To avoid formation of CD73-produced adenosine, several series of potential inhibitors of the target enzyme based on a triazole scaffold were synthetized and evaluated on recombinant purified hCD73 and in cell-based assays.

NURR1 RECEPTOR MODULATORS

Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.

BIOISPIRED PROTEASOME ACTIVATORS WITH ANTIAGEING ACTIVITY

The present invention relates to novel bio-inspired hybrid compounds of formula I which act as proteasome activators and exhibit anti-ageing activity, as well as methods for their synthesis. These hybrid compounds combine the structural features of hydroxytyrosol and the natural antioxidant vitamin E or its bioisosteres in one molecular scaffold. The compounds of formula I, which include structural proteasome activators (activation by stereochemical interaction), can be used in the production of anti-ageing products, such as cosmetic preparations. Additionally, they can be used in conditions and diseases where the proteasome is down-regulated, as well as proteasome-activation control compounds.

Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents

A series of triazoles have been prepared and evaluated as inhibitors of InhA as well as inhibitors of Mycobacterium tuberculosis H37R v. Several of these new compounds possess a good activity against InhA, particularly compounds 17 and 18 for which molecular docking has been performed. Concerning their activities against M. tuberculosis H 37RV strain, two of them, 3 and 12, were found to be good inhibitors with MIC values of 0.50 and 0.25 μg/mL, respectively. Particularly, compound 12 presenting the best MIC value of all compounds tested (0.6 μM) is totally inactive against InhA.

Synthesis and biological evaluation of isosteric analogs of mandipropamid for the control of oomycete pathogens

A series of isosteric analogs of mandipropamid were designed and synthesized via 'click chemistry'. The amide bond of mandipropamid was substituted by a 1,2,3-triazole functional group. The bioassay results have indicated that some of the title compounds exhibited moderate fungicidal activity against Pseudoperonospora cubensis, and the activity has been systematically studied as a function of molecular structure. The low activity of the mandipropamid analog that contains a lipid chain is likely due to the presence of a weak hydrogen bond donor in the 1,2,3-triazole. Furthermore, we have performed the molecular modeling and found that N-methylamide could be more effective than amide as the surrogates to 1,2,3-triazole, which ultimately leads to a longer distance (1.1A longer) between the two substitutes in the 1,4-disubstituted 1,2,3-triazole compound.

Nonafluorobutanesulfonyl azide: A shelf-stable diazo transfer reagent for the synthesis of azides from primary amines

Nonafluorobutanesulfonyl azide is an efficient, shelf-stable and cost-effective diazo transfer reagent for the synthesis of azides from primary amines. The reagent can also be successfully applied to the one-pot regioselective synthesis of 1,2,3-triazoles from primary amines by a sequential diazo transfer and azide-alkyne 1,3-dipolar cycloaddition process catalyzed by copper. The cycloaddition step can be conducted in an inter- or intramolecular way to afford 1,4- or 1,5-disubstituted triazoles, respectively. The atypical 1,5-regioselectivity under copper catalysis is a consequence of geometrical constraints of the amino-alkyne substrates used in the intramolecular version. Nonafluorobutanesulfonyl azide offers an advantageous alternative to the better known and most commonly used trifluoromethanesulfonyl azide.

Copper-in-charcoal-catalyzed, tandem one-pot diazo transfer-click reactions

Copper-in-charcoal (Cu/C) is an effective heterogeneous catalyst for tandem diazo transfer/click reactions. In the presence of Cu/C, various azides can be generated in situ from the corresponding amines, and subsequently undergo [3+ 2] cycloaddition with terminal alkynes to afford triazoles in good yields. The catalyst is also easily recycled.