1609191-08-3

Upstream product

• 49645-27-4 (S)-2-(((benzyloxy)carbonyl)amino)-8-(tert-butoxy)-8-oxooctanoic acid 
• 74-89-5 methylamine 
• 1609191-02-7 (S)-tert-butyl 7-(((benzyloxy)carbonyl)amino)-8-(methoxy(methyl)amino)-8-oxooctanoate 
• 1609191-03-8 (S)-tert-butyl 7-(((benzyloxy)carbonyl)amino)-8-oxooctanoate 
• 1609191-04-9 ⁽⁵⁾-tert-butyl 7-(((benzyloxy)carbonyl)amino)-7-(1H-imidazol-2-yl)heptanoate 
• 1609191-06-1 (S)-tert-butyl 7-(((benzyloxy)carbonyl)amino)-7-(4,5-diiodo-1H-imidazol-2-yl)heptanoate 
• 1609191-05-0 C₂₂H₃₀IN₃O₄ 

Relevant academic research and scientific papers

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs

The identification of a new series of P. falciparum growth inhibitors is described. Starting from a series of known human class I HDAC inhibitors a SAR exploration based on growth inhibitory activity in parasite and human cells-based assays led to the identification of compounds with submicromolar inhibition of P. falciparum growth (EC50 50-fold). Inhibition of parasital HDACs as the mechanism of action of this new class of selective growth inhibitors is supported by hyperacetylation studies.

COMPOUNDS FOR USE IN THE TREATMENT OF PARASITIC DISEASES

The present invention relates to compounds useful for treating parasitic diseases, which are infectious diseases caused or transmitted by a parasite. Compounds of the invention are particularly active against the causative pathogens in malaria. Such compounds are selective inhibitors of parasitic histone deacetylase (PfHDAC) and suppress the growth of parasites, such as Plasmodium falciparum, at a lower concentration than the concentration required for the inhibition of the growth of mammalian cells.