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Issue 6, 2017
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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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Supplementary files

Article information


Submitted
02 Jun 2016
Accepted
03 May 2017
First published
05 May 2017

Med. Chem. Commun., 2017,8, 1275-1282
Article type
Research Article

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, 8, 1275
DOI: 10.1039/C6MD00306K

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