1. Academic Validation
  2. 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

  • J Med Chem. 2010 Nov 25;53(22):8197-201. doi: 10.1021/jm100882t.
Salvatore Bongarzone 1 Hoang Ngoc Ai Tran Andrea Cavalli Marinella Roberti Paolo Carloni Giuseppe Legname Maria Laura Bolognesi
Affiliations

Affiliation

  • 1 Statistical and Biological Physics Sector, Neurobiology Sector, Scuola Internazionale Superiore di Studi Avanzati (SISSA), Via Bonomea 265, 34136 Trieste, Italy.
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-138865
    98.35%, Antiprion Ligand