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Ring-opened aminothienopyridazines as novel tau aggregation inhibitors

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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.

Graphical abstract: Ring-opened aminothienopyridazines as novel tau aggregation inhibitors

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Publication details

The article was received on 02 Jun 2016, accepted on 03 May 2017 and first published on 05 May 2017


Article type: Research Article
DOI: 10.1039/C6MD00306K
Citation: Med. Chem. Commun., 2017, Advance Article
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    Ring-opened aminothienopyridazines as novel tau aggregation inhibitors

    M. Moir, S. W. Chua, T. Reekie, A. D. Martin, A. Ittner, L. M. Ittner and M. Kassiou, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C6MD00306K

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