3094-34-6

Upstream product

• 4083-33-4 2-methyl-4-(4-trifluoromethyl-benzylidene)-4H-oxazol-5-one 
• 455-19-6 4-Trifluoromethylbenzaldehyde 
• 543-24-8 N-acetylglycine 

Downstream Products

• 120658-71-1 2-oxo-3-(4-(trifluoromethyl)phenyl)propanoic acid 
• 1601468-83-0 2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono)-3-(4-(trifluoromethyl)phenyl)propanoic acid 
• 1601468-82-9 2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono)-3-(4-(trifluoromethyl)phenyl)propanoic acid 
• 745018-58-0 2-hydroxy-3-(4-(trifluoromethyl)phenyl)acrylic acid 
• 14091-16-8 4-(trifluoromethyl)-dl-phenylalanine 
• 82337-58-4 2-acetamido-3-(4-(trifluoromethyl)phenyl)propanoic acid 

Relevant academic research and scientific papers

Alpha-amino acrylate microbicide and preparation method and application thereof

The invention provides an alpha-amino acrylate microbicide and a preparation method and application thereof. The alpha-amino acrylate microbicide has a specific chemical structure formula shown as a formula I, and the formula I is shown in the description. The alpha-amino acrylate microbicide has the advantages that by utilizing the design principle of pesticide molecules, a medical leading compound with anti-coronavirus activity is performed with structure modification of agricultural plant virus-resisting activity, a series of alpha-amino acrylate derivatives is designed and synthesized, and particularly, the alpha-amino acrylate derivative containing piperidine ring is synthesized; the known compound is used as a positive reference compound to systematically screen the biology activity; a plurality of high-efficiency anti-virus leading molecules are provided for the developing of new pesticides, and the positive meaning is realized for the reduction application of the pesticide and the protection of environment ecology.

Structure-activity relationship study of 4EGI-1, small molecule eIF4E/eIF4G protein-protein interaction inhibitors

Abstract Protein-protein interactions are critical for regulating the activity of translation initiation factors and multitude of other cellular process, and form the largest block of untapped albeit most challenging targets for drug development. 4EGI-1, (E/Z)-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl) hydrazono)-3-(2-nitrophenyl)propanoic acid, is a hit compound discovered in a screening campaign of small molecule libraries as an inhibitor of translation initiation factors eIF4E and eIF4G protein-protein interaction; it inhibits translation initiation in vitro and in vivo. A series of 4EGI-1-derived thiazol-2-yl hydrazones have been designed and synthesized in order to delineate the structural latitude and improve its binding affinity to eIF4E, and increase its potency in inhibiting the eIF4E/eIF4G interaction. Probing a wide range of substituents on both phenyl rings comprising the 3-phenylpropionic acid and 4-phenylthiazolidine moieties in the context of both E- and Z-isomers of 4EGI-1 led to analogs with enhanced binding affinity and translation initiation inhibitory activities.