Novel Furan-2-yl-1 H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation

Philip Ryan; Mingming Xu; Kousar Jahan; Andrew K. Davey; Prasad V. Bharatam; Shailendra Anoopkumar-Dukie; Michael Kassiou; George D. Mellick; Santosh Rudrawar

doi:10.1021/acschemneuro.0c00252

Novel Furan-2-yl-1 H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation

Philip Ryan, Mingming Xu, Kousar Jahan, Andrew K. Davey, Prasad V. Bharatam, Shailendra Anoopkumar-Dukie, Michael Kassiou, George D. Mellick, Santosh Rudrawar^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	2303-2315
Number of pages	13
Journal	ACS Chemical Neuroscience
Volume	11
Issue number	15
DOIs	https://doi.org/10.1021/acschemneuro.0c00252
Publication status	Published - 5 Aug 2020
Externally published	Yes

Keywords

Molecular modeling studies
Neurodegenerative diseases
Parkinson's disease
aminopyrazole
anle138b
α-Synuclein aggregation

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10.1021/acschemneuro.0c00252

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title = "Novel Furan-2-yl-1 H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation",

abstract = "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.",

keywords = "Molecular modeling studies, Neurodegenerative diseases, Parkinson's disease, aminopyrazole, anle138b, α-Synuclein aggregation",

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year = "2020",

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doi = "10.1021/acschemneuro.0c00252",

language = "English",

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AU - Ryan, Philip

AU - Xu, Mingming

AU - Jahan, Kousar

AU - Davey, Andrew K.

AU - Bharatam, Prasad V.

AU - Anoopkumar-Dukie, Shailendra

AU - Kassiou, Michael

AU - Mellick, George D.

AU - Rudrawar, Santosh

PY - 2020/8/5

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AB - 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.

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Novel Furan-2-yl-1 H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation

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Keywords

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