Format

Send to

Choose Destination
J Med Chem. 2013 Jun 13;56(11):4135-55. doi: 10.1021/jm3017317. Epub 2013 Mar 13.

Progress and developments in tau aggregation inhibitors for Alzheimer disease.

Author information

1
Laboratory of Organic Synthesis of Functional Systems, Humboldt-Universit├Ąt zu Berlin, Brook-Taylor-Strasse 2, 12489 Berlin, Germany. bruno.bulic@huberlin.de

Abstract

Pharmacological approaches directed toward Alzheimer disease are diversifying in parallel with a growing number of promising targets. Investigations on the microtubule-associated protein tau yielded innovative targets backed by recent findings about the central role of tau in numerous neurodegenerative diseases. In this review, we summarize the recent evolution in the development of nonpeptidic small molecules tau aggregation inhibitors (TAGIs) and their advancement toward clinical trials. The compounds are classified according to their chemical structures, providing correlative insights into their pharmacology. Overall, shared structure-activity traits are emerging, as well as specific binding modes related to their ability to engage in hydrogen bonding. Medicinal chemistry efforts on TAGIs together with encouraging in vivo data argue for successful translation to the clinic.

PMID:
23484434
DOI:
10.1021/jm3017317
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center