151133-14-1Relevant articles and documents
An expedient conversion of α-amino acids into Weinreb amides using COMU As a coupling agent
Tyrrell, Elizabeth,Brawn, Peter,Carew, Mark,Greenwood, Iain
experimental part, p. 369 - 372 (2011/02/28)
The use of COMU, as a non-hazardous partner, in the coupling of N-protected α-amino acids to N-methoxy-N-methylamine to afford the corresponding Weinreb amides is discussed. From a practical point of view the reaction can be monitored visually by virtue of the colour change associated with the conversion of substrates (yellow) into the products (orange). As the by-products of the reaction are conveniently water-soluble the products are isolated relatively pure and with minimal racemisation. These factors coupled with the short reaction time make this a very useful procedure.
Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy
Lescop, Cyrille,Herzner, Holger,Siendt, Herve,Bolliger, Reto,Henneboehle, Marco,Weyermann, Philipp,Briguet, Alexandre,Courdier-Fruh, Isabelle,Erb, Michael,Foster, Mark,Meier, Thomas,Magyar, Josef P.,Von Sprecher, Andreas
, p. 5176 - 5181 (2007/10/03)
Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50 values down to 25 nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.
Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors
Palmer, James T.,Rasnick, David,Klaus, Jeffrey L.,Broemme, Dieter
, p. 3193 - 3196 (2007/10/02)
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