Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors

• Tipo: Artigo em Revista Científica Internacional
• Data: 2009

Autores

Asensio Gonzalez (Autor) Outra; Josefina Quirante (Autor) Outra; Joan Nieto (Autor) Outra; Maria Rosario Almeida (Autor) ICBAS; Maria Joao Saraiva (Autor) ICBAS; Antoni Planas (Autor) Outra; Gemma Arsequell (Autor) Outra; Gregorio Valencia (Autor) Outra

Revista

Título: Bioorganic and Medicinal Chemistry Letters

Vol. 19

Páginas: 5270-5273

ISSN: 0960-894X

Editora: Elsevier

Indexação

ISI Web of Knowledge - 36 Citações

Scopus - 44 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-003-FYA

DOI: 10.1016/j.bmcl.2009.03.004

Abstract (EN): The isatin core structure was found to be a novel chemical scaffold in transthyretin (TTR) brillogenesis inhibitor design. Among the series of isatin analogues prepared and tested, the nitro compound 1,3-dihydro3-[(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. (C) 2009 Published by Elsevier Ltd.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 4