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Published on: June 23, 2019
QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors
Kyung Ah Koo1, Nam Doo Kim, Yong Sog Chon
1Biohealth Products Research Center, Inje University, Gimhae, Gyongnam, South Korea.
Abstract:
Individuals with Down syndrome (DS) suffer from mental retardation. Overexpression and the resulting increased specific activity of Dyrk1A kinase located on chromosome 21 cause a learning and memory deficit in Dyrk1A transgenic mice. To search for therapeutic agents with Dyrk1A inhibition activity, previously we obtained HCD160 as a new hit compound for Dyrk1A inhibition. In the present study, we synthesized 34 HCD160 derivatives to investigate the quantitative structure-activity relationship (QSAR). This analysis could provide important information for novel drug discovery for treatment of DS related learning and memory deficits.
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