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Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

ABSTRACT: 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 related cysteine protease, rhodesain.

SUBMITTER: Chen YT 

PROVIDER: S-EPMC2642929 | biostudies-literature | 2008 Nov

REPOSITORIES: biostudies-literature

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Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

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]

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