119920-86-4Relevant academic research and scientific papers
Difluoromethyleneketone retroamide, a versatile concept of inactivation of proteolytic enzymes
Schirlin,Baltzer,Altenburger,Tarnus,Remy
, p. 305 - 318 (2007/10/02)
The synthesis of difluoromethyleneketone retroamides is described. Several examples of application to aspartyl or seryl proteases illustrate the versatility of this inactivation concept. Copyright
General Synthesis of Polyfunctionalized Fluoromethyleneketone Retroamides as Potential Inhibitors of Thrombin
Altenburger, J. M.,Schirlin, D.
, p. 7255 - 7258 (2007/10/02)
Synthesis of polyfunctionalized fluoromethyleneketone retroamides is described.A potential inhibitor of human Thrombin has been prepared through a Reformatsky type condensation from N-protected p-NO2 phenylalaninal.The reaction conditions are applicable t
Novel peptidase inhibitors
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, (2008/06/13)
This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide bond of a partial retropeptide analog of the substrate has been replaced by a difluoromethylene moiety. These peptidase substrate analogs provide specific enzyme inhibitors for a variety of proteases, the inhibition of which exert valuable pharmacological activities and therefore have useful physiological consequences in a variety of disease states.
A CONVENIENT SYNTHESIS OF &α',&β-DIAMINO- &α,&α-DIFLUOROKETONES, NEW DIPEPTIDE ISOSTERES
Schirlin, D.,Baltzer, S.,Altenburger, J. M.
, p. 3687 - 3690 (2007/10/02)
A convenient and versatile synthesis of α',β-diamino-α,α-difluoroketones is described.These compounds represent a new class of true dipeptide isosteres useful for the design of serine protease inhibitors.
Novel peptidase inhibitors
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, (2008/06/13)
This invention relates to activated electrophilic ketone retroamide analogs of certain peptidase substrates having the formula R1NHCHR2COCF2CHR3(NRbCOXRa)nQ These compounds are useful in inhibiting serine-, thiol-, carboxylic acid- and metallo- dependent
