913094-50-5Relevant academic research and scientific papers
CYCLIC KETO-AMIDE COMPOUNDS AS CALPAIN MODULATORS AND METHODS OF PRODUCTION AND USE THEREOF
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Paragraph 00375; 00376, (2017/09/27)
The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer whic
Design and evaluation of Trypanosoma brucei metacaspase inhibitors
Berg, Maya,Veken, Pieter Van der,Joossens, Jurgen,Muthusamy, Venkatraj,Breugelmans, Matthias,Moss, Catherine X.,Rudolf, Jana,Cos, Paul,Coombs, Graham H.,Maes, Louis,Haemers, Achiel,Mottram, Jeremy C.,Augustyns, Koen
scheme or table, p. 2001 - 2006 (2010/10/01)
Metacaspase (MCA) is an important enzyme in Trypanosoma brucei, absent from humans and differing significantly from the orthologous human caspases. Therefore MCA constitutes a new attractive drug target for antiparasitic chemotherapeutics, which needs further characterization to support the discovery of innovative drug candidates. A first series of inhibitors has been prepared on the basis of known substrate specificity and the predicted catalytic mechanism of the enzyme. In this Letter we present the first inhibitors of TbMCA2 with low micromolar enzymatic and antiparasitic activity in vitro combined with low cytotoxicity.
Practical total syntheses of epiquinamide enantiomers
Suyama, Takashi L.,Gerwick, William H.
, p. 4541 - 4543 (2007/10/03)
Short and practical syntheses of epiquinamide and its enantiomer were accomplished with high overall yields and high stereoselectivity from readily available starting materials. American Chemical Society.
