Ontology highlight
ABSTRACT:
SUBMITTER: Neitz RJ
PROVIDER: S-EPMC4737481 | biostudies-literature | 2015 Nov
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20150623 21
Inhibition of the cysteine protease cruzain from Trypanosoma cruzi has been studied pre-clinically as a new chemotherapeutic approach to treat Chagas' disease. Efficacious effects of vinylsulfone-based cruzain inhibitors in animal models support this therapeutic hypothesis. More recently, substrate-activity screening was used to identify nonpeptidic tetrafluorophenoxymethyl ketone inhibitors of cruzain that showed promising efficacy in animal models. Herein we report efforts to further optimize ...[more]