106746-07-0Relevant articles and documents
Base-catalysed 18F-labelling of trifluoromethyl ketones. Application to the synthesis of 18F-labelled neutrophil elastase inhibitors
Meyer, Denise N.,Cortés González, Miguel A.,Jiang, Xingguo,Johansson-Holm, Linus,Pourghasemi Lati, Monireh,Elgland, Mathias,Nordeman, Patrik,Antoni, Gunnar,Szabó, Kálmán J.
supporting information, p. 8476 - 8479 (2021/09/02)
A new method for the fluorine-18 labelling of trifluoromethyl ketones has been developed. This method is based on the conversion of a-COCF3 functional group to a difluoro enol silyl ether followed by halogenation and fluorine-18 labelling. The utility of this new method was demonstrated by the synthesis of fluorine-18 labelled neutrophil elastase inhibitors, which are potentially useful for detection of inflammatory disorders.
Peptidase inhibitors
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, (2008/06/13)
This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
Synthesis of peptidyl fluoromethyl ketones and peptidyl α-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G
Peet,Burkhart,Angelastro,Giroux,Mehdi,Bey,Kolb,Neises,Schirlin
, p. 394 - 407 (2007/10/02)
Comparison of MeO-Suc-Val-Pro-Phe-CO2Me (29) and MeO-Suc-Ala-Ala-Pro-Phe-CO2Me (25) with their corresponding trifluoromethyl ketones 9a and 9b, respectively, in rat and human neutrophil cathepsin G assays showed the α-keto esters to