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A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.

Abstract：

:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Simões CJV,Almeida ZL,Costa D,Jesus CSH,Cardoso AL,Almeida MR,Saraiva MJ,Pinho E Melo TMVD,Brito RMM

doi

10.1016/j.ejmech.2016.02.074

subject

Has Abstract

pub_date

2016-10-04 00:00:00

pages

823-840

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30174-X

journal_volume

121

pub_type

杂志文章

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