Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors.

Article Details

Citation

Copy to clipboard

Gonzalez A, Quirante J, Nieto J, Almeida MR, Saraiva MJ, Planas A, Arsequell G, Valencia G

Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5270-3. doi: 10.1016/j.bmcl.2009.03.004. Epub 2009 Mar 6.

PubMed ID

19651509 [ View in PubMed

]

Abstract

The isatin core structure was found to be a novel chemical scaffold in transthyretin (TTR) fibrillogenesis inhibitor design. Among the series of isatin analogues prepared and tested, the nitro compound 1,3-dihydro-3-[(4-nitrophenyl)imino]-2H-indol-2-one (2r) is as potent as triiodophenol, which is one of the most active known TTR inhibitors. The E/Z stereochemistry of these molecules in solution, elucidated by (1)H NMR, does not influence their biological activity. The compounds do not bind to the native tetrameric TTR suggesting that their inhibitory action is independent of the protein binding and stabilization.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Levothyroxine	Transthyretin	IC 50 (nM)	10500	N/A	N/A	Details