Ring-opened aminothienopyridazines as novel tau aggregation inhibitors

M. Moir, S. W. Chua, T. Reekie, A. D. Martin, A. Ittner, L. M. Ittner, M. Kassiou

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

Abstract

Aminothienopyridazines (ATPZs) have demonstrated efficacy, in vitro, as tau protein aggregation inhibitors. Modifications were made to the ATPZ scaffold to determine the importance of certain structural features for activity. More specifically, ring-opened analogues detached at the nitrogen-nitrogen bond of the pyridazine, were synthesized and their inhibitory activity evaluated. Preliminary data suggests that the ring-opened structures retain inhibitory activity, independent of tau oxidation. The structures detailed represent the beginnings of a deconstruction-reconstruction-elaboration study, with the aim of identifying simpler scaffolds, which retain activity and can be optimized in terms of physiochemical properties.

Original languageEnglish
Pages (from-to)1275-1282
Number of pages8
JournalMedChemComm
Volume8
Issue number6
DOIs
Publication statusPublished - Jun 2017
Externally publishedYes

Keywords

  • Aminothienopyridazines (ATPZs
  • Alzheimer's disease
  • tau protein aggregation inhibitors

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