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Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation
Author(s) -
Philip Ryan,
Mingming Xu,
Kousar Jahan,
Andrew K. Davey,
Prasad V. Bharatam,
Shailendra AnoopkumarDukie,
Michael Kassiou,
George D. Mellick,
Santosh Rudrawar
Publication year - 2020
Publication title -
acs chemical neuroscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.158
H-Index - 69
ISSN - 1948-7193
DOI - 10.1021/acschemneuro.0c00252
Subject(s) - furan , chemistry , in vitro , pharmacology , stereochemistry , inhibitory postsynaptic potential , structure–activity relationship , biochemistry , biology , neuroscience , organic chemistry
A series of novel furan-2-yl-1 H -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.

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