127977-24-6Relevant articles and documents
Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes
Jaishankar, Priyadarshini,Hansell, Elizabeth,Zhao, Dong-Mei,Doyle, Patricia S.,McKerrow, James H.,Renslo, Adam R.
, p. 624 - 628 (2008/09/16)
A systematic study of P2 and P3 substitution in a series of vinyl sulfone cysteine protease inhibitors is described. The introduction of a methyl substituent in the P2 phenylalanine aryl ring had a favorable effect on protease inhibition and conferred modest selectivity for rhodesain over cruzain. Rhodesain selectivity could be enhanced further by combining these P2 modifications with certain P3 amide substituents.
SYNTHESIS OF ENANTIOMERICALLY PURE PROTECTED β-ARYL ALANINES
Jackson, Richard F. W.,Wythes, Martin J.,Wood, Anthony
, p. 5941 - 5944 (2007/10/02)
The organozinc reagent (1), prepared from the β-iodoalanine derivative (2), reacts with aryl iodides at 50 deg C in the presence of catalytic bis(tri-o-tolylphosphine)palladium dichloride to give in moderate to good yields enantiomerically pure protected