714963-55-0

Upstream product

• 209991-63-9 2,4,6-trifluorophenylacetic acid 

Downstream Products

• 1619924-36-5 C₁₉H₁₉F₂N₅ 
• 716324-86-6 6,8-dichloro-7-(2,4,6-trifluorophenyl)pyrido[2,3-b]pyrazine 
• 716324-85-5 8-hydroxy-7-(2,4,6-trifluorophenyl)pyrido[2,3-b]pyrazin-6(5H)-one 
• 1447018-16-7 2-(benzylthio)-6-(2-bromo-6-(2-(4-methoxyphenyl)acetamido)benzamido)-N-methylbenzamide 
• 1447018-14-5 2-(benzylthio)-6-(2-bromo-6-(2-(2,4,6-trifluorophenyl)acetamido)benzamido)-N-methylbenzamide 
• 1444387-00-1 C₂₅H₂₅F₃N₆O₂ 
• 872088-75-0 6-(4-fluorophenyl)-3-[2-(2,4,6-trifluorophenyl)-acetylamino]-pyrazine-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

Phosphonic acid analogs of fluorophenylalanines as inhibitors of human and porcine aminopeptidases N: Validation of the importance of the substitution of the aromatic ring

A library of phosphonic acid analogs of phenylalanine substituted with fluorine, chlorine and trifluoromethyl moieties on the aromatic ring was synthesized and evaluated for inhibitory activity against human (hAPN) and porcine (pAPN) aminopeptidases. Fluorogenic screening indicated that these analogs are micromolar or submicromolar inhibitors, both enzymes being more active against hAPN. In order to better understand the mode of the action of the most active compounds, molecular modeling was used. It confirmed that aminophosphonic portion of the enzyme is bound nearly identically in the case of all the studied compounds, whereas the difference in activity results from the placement of aromatic side chain of an inhibitor. Interestingly, both enantiomers of the individual compounds are usually bound quite similarly.

HETEROCYCLIC COMPOUNDS AND THEIR USE FOR THE TREATMENT OF NEURODEGENERATIVE TAUOPATHIES

The present invention is directed to triazolopyrimidine, phenylpyrimidine, pyridopyridazine, and pyridotriazine compounds and their use in the treatment of neurodegenerative disorders.

Design, synthesis and insecticidal activity of novel anthranilic diamides with benzyl sulfide scaffold

A series of novel anthranilic diamides with benzyl sulfide scaffold were synthesized, in which N-pyridylpyrazole moiety generally regarded as key pharmacophore was abandoned. The target compounds were characterized by 1H NMR, 13C NMR, 19F NMR and HRMS. The preliminary bioassays indicated that half of the title compounds were endowed with good insecticidal activities against armyworm (Mythimna sepatara) at the concentration of 500 mg/L. Exhilaratingly, the synthesized compound 3a was also active against Tetranychus cinnabarinus at 100 mg/L. The difference in activities between the target compounds was influenced by the substituents, which provided some hints for further investigation on structure modifications.

The human Aurora kinase inhibitor danusertib is a lead compound for anti-trypanosomal drug discovery via target repurposing

New drugs for neglected tropical diseases such as human African trypanosomiasis (HAT) are needed, yet drug discovery efforts are not often focused on this area due to cost. Target repurposing, achieved by the matching of essential parasite enzymes to those human enzymes that have been successfully inhibited by small molecule drugs, provides an attractive means by which new drug optimization programs can be pragmatically initiated. In this report we describe our results in repurposing an established class of human Aurora kinase inhibitors, typified by danusertib (1), which we have observed to be an inhibitor of trypanosomal Aurora kinase 1 (TbAUK1) and effective in parasite killing in vitro. Informed by homology modeling and docking, a series of analogs of 1 were prepared that explored the scope of the chemotype and provided a nearly 25-fold improvement in cellular selectivity for parasite cells over human cells.

PYRIDODIAZINES AS PLANT FUNGICIDES

Fungicidal compounds of general formula (1) wherein R, R1, R2, W, X, Y and Z are as defined in the specification.