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

Ryan, Philip ; Xu, Mingming ; Jahan, Kousar ; Davey, Andrew K. ; Bharatam, Prasad V. ; Anoopkumar-Dukie, Shailendra ; Kassiou, Michael ; Mellick, George D. ; Rudrawar, Santosh (2020) Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation ACS Chemical Neuroscience, 11 (15). pp. 2303-2315. ISSN 1948-7193

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Official URL: http://doi.org/10.1021/acschemneuro.0c00252

Related URL: http://dx.doi.org/10.1021/acschemneuro.0c00252

Abstract

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.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society.
Keywords:Α-synuclein Aggregation; Parkinson’s Disease; Neurodegenerative Diseases; Anle138b; Molecular Modeling Studies; Aminopyrazole.
ID Code:116253
Deposited On:12 Apr 2021 08:36
Last Modified:12 Apr 2021 08:36

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