28317-60-4

Upstream product

• 1118-61-2 3-Aminocrotononitrile 
• 108-42-9 3-chloro-aniline 

Downstream Products

• 123534-21-4 1-(m-chlorophenyl)-1,6-dihydro-6-oxo-4-styrylpyridazin-3,5-dicarbonitrile 
• 123534-22-5 1-(3-Chloro-phenyl)-4-[(E)-2-(4-chloro-phenyl)-vinyl]-6-oxo-1,6-dihydro-pyridazine-3,5-dicarbonitrile 
• 123534-14-5 8-Amino-2-(3-chloro-phenyl)-6-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-cinnoline-4,7-dicarbonitrile 
• 123534-11-2 1-(3-Chloro-phenyl)-4-methyl-6-oxo-1,6-dihydro-pyridazine-3,5-dicarbonitrile 

Relevant academic research and scientific papers

Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and related derivatives

A FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2b), showing an IC50 value of 50 μM. For a preliminary assessment of their antivirulence properties the new derivatives were tested for their antibiofilm activity. The most active compound resulted 2a, which showed inhibition of about 60% against S. aureus ATCC 29213, S. aureus ATCC 25923, S. aureus ATCC 6538 and S. epidermidis RP62A at a screening concentration of 100 μM.