Novel furan-2-yl-1H-pyrazoles possess inhibitory activity against α-synuclein aggregation
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Xu, M
Jahan, K
Davey, AK
Bharatam, PV
Anoopkumar-Dukie, S
Kassiou, M
Mellick, GD
Rudrawar, S
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Abstract
A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesised and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation. 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.
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ACS Chemical Neuroscience
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DE140101632
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This document is the Postprintof a Published Work that appeared in final form in ACS Chemical Neuroscience, © YEAR American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acschemneuro.0c00252
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Medicinal and biomolecular chemistry
Biochemistry and cell biology
Analytical chemistry
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Ryan, P; Xu, M; Jahan, K; Davey, AK; Bharatam, PV; Anoopkumar-Dukie, S; Kassiou, M; Mellick, GD; Rudrawar, S, Novel furan-2-yl-1H-pyrazoles possess inhibitory activity against α-synuclein aggregation, ACS Chemical Neuroscience, 2020