887035-89-4

Usage

Uses

1-(4-Fluoro-phenyl)-5-methyl-1h-[1,2,3]triazole-4-carboxylic acid

Upstream product

• 3296-02-4 p-azidofluorobenzene 
• 141-97-9 ethyl acetoacetate 
• 1182710-58-2 C₁₀H₈FN₃O 
• 371-40-4 4-fluoroaniline 
• 1147216-22-5 1-(4-fluoro-phenyl)-5-methyl-1H-[1,2,3]triazole-4-carboxylic acid ethyl ester 
• 1765-93-1 4-fluoroboronic acid 
• 1182710-57-1 C₁₀H₁₀FN₃O 

Downstream Products

• 1159000-59-5 C₁₀H₇ClFN₃O 
• 1182710-56-0 C₂₅H₂₂FN₅O₄S 
• 1147216-22-5 1-(4-fluoro-phenyl)-5-methyl-1H-[1,2,3]triazole-4-carboxylic acid ethyl ester 
• 1187324-59-9 1-(4-fluorophenyl)-5-methyl-N-(6-methyl-2-pyridinyl)-1H-1,2,3-triazole-4-carboxamide 
• 1187324-77-1 1-(4-fluorophenyl)-5-methyl-N-(4-methyl-2-pyrimidinyl)-1H-1,2,3-triazole-4-carboxamide 
• 1147206-25-4 methyl 1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazole-4-carboxylate 
• 1410806-51-7 1-(1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl)-2-(pyrrolidin-1-yl)ethanone 
• 1410806-89-1 2-chloro-1-[1-(4-fluoro-phenyl)-5-methyl-1H-[1,2,3]triazol-4-yl]-ethanone 
• 1586765-19-6 1-[5-methyl-1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-7-methoxy-4,9-dihydro-3H-β-carboline 
• 1187324-79-3 1-(4-fluorophenyl)-5-methyl-N-(6-methyl-4-pyrimidinyl)-1H-1,2,3-triazole-4-carboxamide 
• 1187324-78-2 N-(4-chloro-2-pyrimidinyl)-1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazole-4-carboxamide 

Relevant academic research and scientific papers

Discovery of novel pyrrolopyrimidine/pyrazolopyrimidine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors

Six series of pyrrolo[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives bearing 1,2,3-triazole moiety were designed and synthesized, and some bio-evaluation was also carried out. As a result, four points can be summarized: Firstly, some of compounds exhibited excellent cytotoxicity activity and selectivity with the IC50 values in single-digit μm level. In particular, the most promising compound 16d showed equal activity to lead compound foretinib against A549, HepG2, and MCF-7 cell lines, with the IC50 values of 4.79?±?0.82, 2.03?±?0.39, and 2.90?±?0.43?μm, respectively. Secondly, the SARs and docking studies indicated that the in vitro antitumor activity of pyrrolo[2,3-d]pyrimidine derivatives bearing 1,2,3-triazole moiety was superior to the pyrazolo[3,4-d]pyrimidine derivatives bearing 1,2,3-triazole moiety. Thirdly, three selected compounds (16d, 18d, and 20d) were further evaluated for inhibitory activity against the c-Met kinase, and the 16d could inhibit the c-Met kinase selectively by experiments of enzyme-based selectivity. What is more, 16d could induce apoptosis of HepG2 cells and inhibitor the cell cycle of HepG2 on G2/M phase by acridine orange staining and cell cycle experiments, respectively.

Synthesis and antibacterial activity of di-heteryl substitued [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazoles

A new series of 3-(5-methyl-1-phenyl-1H-4-pyrazolyl)-6-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo [3,4-b][1,3,4]thiadiazoles 12a-j have been prepared and assayed for their antibacterial activity against human pathogenic Gram-positive bacteria viz., Staphylococcus aureus, Bacillus subtilis and Gram-negative Escherichia coli. Among the screened compounds 12b, 12c and 12f, in which phenyl ring of triazole moiety bear 4-chloro, 4-nitro and 4-fluoro substituents respectively, showed high activity against all the micro-organisms employed. The activities of these compounds are almost equal to the standards.

Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors

A series of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 4 cancer cell lines (HT-29, A549, MCF-7, and PC-3) in vitro. Most compounds showed moderate to excellent potency, with the most promising analog 34 showing a c-Met IC50value of 1.68?nM. Structure–activity relationship studies indicated that electron-withdrawing groups (X?=?CF3, R1?=?F, R2?=?4-F) were required to decrease the higher electron density on the 5-atom linker to a proper degree to improve the inhibitory activity.

PROTEOSTASIS REGULATORS

The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

TRIAZOLES AND PROCESSES FOR PRODUCING THE SAME

The present disclosure relates to triazoles and processes for their preparation. The processes involve a target-guided synthesis approach, whereby an alkyne and an azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the triazole.

Synthesis of 1,2,4- and 1,3,4-oxadiazoles from 1-aryl-5-methyl-1H-1,2,3- triazole-4-carbonyl chlorides

5-Substituted 2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazoles were synthesized by reaction of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonyl chlorides with the corresponding 5-substituted 1H-tetrazoles. 5-Methyl-1-phenyl-1H-1,2,3-triazole-4-carb