Tuning transthyretin amyloidosis inhibition properties of iododiflunisal by combinatorial engineering of the nonsalicylic ring substitutions

Maria Vilaró, Joan Nieto, Juan Ramón La Parra, Maria Rosário Almeida, Alfredo Ballesteros, Antoni Planas, Gemma Arsequell, Gregorio Valencia

Producció científica: Article en revista indexadaArticleAvaluat per experts

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Resum

Two series of iododiflunisal and diflunisal analogues have been obtained by using a two step sequential reaction solution-phase parallel synthesis. The synthesis combined an aqueous Suzuki-Miyaura cross-coupling and a mild electrophilic aromatic iodination step using a new polymer-supported iodonium version of Barluengas reagent. From a selected set of 77 noniodinated and 77 iodinated diflunisal analogues, a subset of good transthyretin amyloid inhibitors has been obtained with improved turbidimetry inhibition constants, high binding affinity to transthyretin, and good selectivity for TTR compared to other thyroxine binding proteins.

Idioma originalAnglès
Pàgines (de-a)32-38
Nombre de pàgines7
RevistaACS Combinatorial Science
Volum17
Número1
DOIs
Estat de la publicacióPublicada - 12 de gen. 2015

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