Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation.,ACS Chemical Neuroscience

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Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation.
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2020-06-18 , DOI: 10.1021/acschemneuro.0c00252
Philip Ryan _{1,

2,

3} , Mingming Xu ₄ , Kousar Jahan ₅ , Andrew K Davey _{1,

2,

3} , Prasad V Bharatam ₅ , Shailendra Anoopkumar-Dukie _{1,

2} , Michael Kassiou ₆ , George D Mellick ₄ , Santosh Rudrawar _{1,

2,

3}

Affiliation

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.

中文翻译：

新型呋喃-2-基-1H-吡唑具有针对α-突触核蛋白聚集的抑制活性。

合成了一系列新型的呋喃-2-基-1 H-吡唑及其化学前体，并评估了它们在体外破坏α-突触核蛋白（α-syn）聚集的功效。发现该化合物抑制α-syn的聚集，其功效与有前途的候选药物anle138b相当。这项研究的结果表明，化合物8b，8l和9f可以作为结构-活性关系研究的次要线索，这些研究旨在确定合适的化合物，以改善针对与帕金森氏病有关的α-syn自组装的调节活性。

更新日期：2020-08-05

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