796049-30-4Relevant academic research and scientific papers
Synthesis of analogues of Congo red and evaluation of their anti-prion activity
Sellarajah, Shane,Lekishvili, Tamuna,Bowring, Claire,Thompsett, Andrew R.,Rudyk, Helene,Birkett, Christopher R.,Brown, David R.,Gilbert, Ian H.
, p. 5515 - 5534 (2004)
No cure as of yet exists for any of the transmissible spongiform encephalopathies. In this paper, we describe the synthesis of analogues of Congo red and evaluation against a cellular model of infection, the SMB (scrapie mouse brain) persistently infected cell line, for their ability to inhibit the infectivity of the abnormal form of prion protein (PrP-res). The compounds have also been tested for their ability to inhibit the polymerization of PrP C by PrP-res. A number of analogues showed inhibition of PrP-res infectivity at nanomolar concentrations. Several analogues show promise; the most active compound, 2a, inhibits the formation of PrP-res in SMB cells with an EC50 of 25-50 nM.
