Ryan Philip, Xu Mingming, Jahan Kousar, Davey Andrew K, Bharatam Prasad V, Anoopkumar-Dukie Shailendra, Kassiou Michael, Mellick George D, Rudrawar Santosh
School of Pharmacy and Pharmacology, Griffith University, Gold Coast, Queensland 4222, Australia.
Quality Use of Medicines Network, Griffith University, Gold Coast, Queensland 4222, Australia.
ACS Chem Neurosci. 2020 Aug 5;11(15):2303-2315. doi: 10.1021/acschemneuro.0c00252. Epub 2020 Jul 8.
A series of novel furan-2-yl-1-pyrazoles and their chemical precursors were synthesized 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 , , and 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.
合成了一系列新型呋喃-2-基-1-吡唑及其化学前体，并评估了它们在破坏α-突触核蛋白（α-syn）聚集方面的有效性。发现这些化合物抑制α-syn聚集的效果与有前景的候选药物anle138b相当。这项研究的结果表明，化合物、和可能有资格作为构效关系研究的二级先导物，旨在确定适合改善与帕金森病相关的针对α-syn自组装的调节活性的化合物。
