Novel Furan-2-yl‑1H‑pyrazoles Possess Inhibitory Activity against α‑Synuclein Aggregation

A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesized and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation in vitro. The compounds were found to inhibit α-syn aggregation with efficacy comparable to the promising drug candidate anle13...

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Bibliographic Details
Published in:ACS chemical neuroscience 2020-08, Vol.11 (15), p.2303-2315
Main Authors: Ryan, Philip, Xu, Mingming, Jahan, Kousar, Davey, Andrew K, Bharatam, Prasad V, Anoopkumar-Dukie, Shailendra, Kassiou, Michael, Mellick, George D, Rudrawar, Santosh
Format: Article
Language:English
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Summary:A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesized and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation in vitro. The compounds were found to inhibit α-syn aggregation with efficacy comparable to the promising drug candidate anle138b. The results of this study indicate that compounds 8b, 8l, and 9f may qualify as secondary leads for the structure–activity relationship studies aimed to identify the suitable compounds for improving the modulatory activity targeted at α-syn self-assembly related to Parkinson’s disease.
ISSN:1948-7193
1948-7193
DOI:10.1021/acschemneuro.0c00252