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.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom