Title

Progress and developments in tau aggregation inhibitors for Alzheimer disease.

Journal

Journal of medicinal chemistry

Volume

56

Issue

None

Pages

4135-55

Date

2013-06-13

Authors

Bulic B | Pickhardt M | Mandelkow E

Structures of Aβ-aggregation inhibitors evaluated in current or past clinical trials.

Aminothienopyridazines (APTZs) Tau aggregation inhibitors (B/P: blood to plasma ratio).

Pyrogallol generic substitution pattern commonly found in multiple polyphenolic Tau aggregation inhibitors such as 12 and 19. Note the structural overlap with the inactive pyrocatechol-substituted epicatechin

Redox cycling of methylene blue and TAGI potencies. Upper panel (black): Reduced leuco form 2 and structural overlap with inactive phenothiazines 3, 4, and 5. Lower panel (blue): Structural overlap between oxidized form 1 and azure A (6), reduced anthraquinone, 8, and 9, showing the extended π-conjugated system (ND: not determined).

Representative examples of N-phenylamine Tau aggregation inhibitors and structural overlap with the Aβ40 aggregation inhibitor 33 or the nonsteroidal anti-inflammatory drug 34.

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