Ontology highlight
ABSTRACT:
SUBMITTER: Chen YT
PROVIDER: S-EPMC2642929 | biostudies-literature | 2008 Nov
REPOSITORIES: biostudies-literature
Chen Yen Ting YT Lira Ricardo R Hansell Elizabeth E McKerrow James H JH Roush William R WR
Bioorganic & medicinal chemistry letters 20080610 22
The importance of cysteine proteases in parasites, compounded with the lack of redundancy compared to their mammalian hosts makes proteases attractive targets for the development of new therapeutic agents. The binding mode of K11002 to cruzain, the major cysteine protease of Trypanosoma cruzi was used in the design of conformationally constrained inhibitors. Vinyl sulfone-containing macrocycles were synthesized via olefin ring-closing metathesis and evaluated against cruzain and the closely rela ...[more]