1195124-07-2Relevant articles and documents
Design, synthesis, and structure - Activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease
Thompson, Mark J.,Borsenberger, Vinciane,Louth, Jennifer C.,Judd, Katie E.,Chen, Beining
, p. 7503 - 7511 (2009)
Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders. 2009 American Chemical Society.
