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Parallel Synthesis, Evaluation, and Preliminary Structure-Activity Relationship of 2,5-diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound

Parallel Synthesis, Evaluation, and Preliminary Structure-Activity Relationship of 2,5-diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound

Salvatore Bongarzone, Hoang Ngoc Ai Tran, Andrea Cavalli, Marinella Roberti, Paolo Carloni, Giuseppe Legname, Maria Laura Bolognesi

J Med Chem. 2010 Nov 25;53(22):8197-201.

PMID: 21047125

Abstract:

A library of 11 entries, featuring a 2,5-diamino-1,4-benzoquinones nucleus as spacer connecting two aromatic prion recognition motifs, was designed and evaluated against prion infection. Notably, 6-chloro-1,2,3,4-tetrahydroacridine 10 showed an EC(50) of 0.17 μM, which was lower than that displayed by reference compound BiCappa. More importantly, 10 possessed the capability to contrast prion fibril formation and oxidative stress, together with a low cytotoxicity. This study further corroborates the bivalent strategy as a viable approach to the rational design of anti-prion chemical probes.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP119662554	BiCAPPA		119662-55-4	Price

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