7653-42-1

Upstream product

• 7466-54-8 2-methoxybenzoylhydrazine 
• 333-20-0 potassium thioacyanate 
• 579-75-9 2-Methoxybenzoic acid 
• 606-45-1 2-methoxybenzoic acid methyl ester 
• 1147550-11-5 ammonium thiocyanate 
• 2290-65-5 trimethylsilyl isothiocyanate 
• 79-19-6 thiosemicarbazide 
• 21615-34-9 2-Methoxybenzoyl chloride 

Downstream Products

• 5711-59-1 2-amino-5-(2-methoxyphenyl)-1,3,4-oxadiazole 
• 1276032-85-9 5-o-methoxyphenyl-3-(β-D-glucopyranosylthio)-1,2,4-triazole 
• 1276032-75-7 5-o-methoxyphenyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosylthio)-1,2,4-triazole 
• 114361-97-6 5-(p-nitrophenacylthio)-3-o-methoxyphenyl-s-triazole 
• 114362-03-7 2-(o-methoxyphenyl)-5-(p-nitrophenyl)thiazolo-<3,2-b>-s-triazole 
• 114361-95-4 5-(p-bromophenacylthio)-3-o-methoxyphenyl-s-triazole 
• 114361-96-5 5-(-p-chlorophenacylthio)-3-o-methoxyphenyl-s-triazole 
• 114362-10-6 3-(o-methoxyphenyl)-5-(p-bromophenyl)thiazolo<2,3-c>-s-triazole 
• 114362-01-5 2-(o-methoxyphenyl)-5-(p-bromophenyl)thiazolo<3,2-b>-s-triazole 
• 114362-02-6 2-(o-methoxyphenyl)-5-(p-chlorophenyl)thiazolo-<3,2-b>-s-triazole 
• 39631-37-3 3-(o-methoxyphenyl)-5-mercapto-4H-1,2,4-triazole 
• 114362-08-2 2-(o-methoxybenzoylhydrazino)-4-(p-bromophenyl)-thiazole 

Relevant academic research and scientific papers

Development of phenyltriazole thiol-based derivatives as highly potent inhibitors of DCN1-UBC12 interaction

Defective in cullin neddylation 1(DCN1) is a co-E3 ligase that is important for cullin neddylation. Dysregulation of DCN1 highly correlates with the development of various cancers. Herein, from the initial high-throughput screening, a novel hit compound 5a containing a phenyltriazole thiol core (IC50 value of 0.95 μM for DCN1-UBC12 interaction) was discovered. Further structure-based optimization leads to the development of SK-464 (IC50 value of 26 nM). We found that SK-464 not only directly bound to DCN1 in vitro, but also engaged cellular DCN1, suppressed the neddylation of cullin3, and hindered the migration and invasion of two DCN1-overexpressed squamous carcinoma cell lines (KYSE70 and H2170). These findings indicate that SK-464 may be a novel lead compound targeting DCN1-UBC12 interaction.

Mild and convenient one-pot synthesis of 2-amino-1,3,4-oxadiazoles promoted by trimethylsilyl isothiocyanate (TMSNCS)

A mild, convenient, and efficient one-pot synthesis of amino-1,3,4- oxadiazoles is described. In situ preparation of various thiosemicarbazides by the reaction of different carboxylic acid hydrazides with trimethylsilyl isothiocyanate (TMSNCS), followed by cyclodesulfurization of thiosemicarbazides under basic conditions in the presence of I2/KI resulted in 2-amino-1,3,4-oxadiazoles in high yields (79-94%).

Trimethylsilyl isothiocyanate (TMSNCS): An efficient reagent for the one-pot synthesis of mercapto-1,2,4-triazoles

A mild, convenient, and efficient one-pot synthesis of mercapto-1,2,4- triazoles is described. Various hydrazides efficiently reacted with trimethylsilyl isothiocyanate (TMSNCS) under basic condition to give mercapto-1,2,4-triazoles in high yields.

Synthesis and antibacterial activities of new S-glycosides bearing 1,2,4-triazole

Several new 5-aryl-3-(β-D-glucopyranosylthio)-1,2,4-triazoles have been synthesized. The structures of these new compounds were confirmed by 1H NMR, 13C NMR and elemental analyses.The antibacterial activities of the compounds were also evaluated.

GLUCOKINASE ACTIVATORS

Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

Heterocyclic Systems Containing Bridgehead Nitrogen Atom: Part LVII-Syntheses of 2,5-Disubstituted Thiazolo-s-triazoles and 3,5-Disubstituted Thiazolo-s-triazoles

5-Mercapto-3-substituted-s-triazoles (III, R1 = o-MeOC6H4, R1 = o-BrC6H4) on reaction with α-halogenoketones in anhyd. ethanol give ketones (IVa-a2, IVb-b3) which on cyclization with polyphosphoric acid (PPA) furnish the respective thiazolo-s-triaz