1011726-50-3Relevant 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.