1234351-86-0Relevant articles and documents
Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors
Lee, Young Hun,Shin, Min Cheol,Yun, Yong Don,Shin, Seo Young,Kim, Jong Min,Seo, Jeong Moo,Kim, Nam-Jung,Ryu, Jong Hoon,Lee, Yong Sup
, p. 231 - 240 (2015)
Alzheimer's disease (AD), a progressive and neurodegenerative disorder of the brain, is the most common cause of dementia among elderly people. To date, the successful therapeutic strategy to treat AD is maintaining the levels of acetylcholine by inhibiting acetylcholinesterase (AChE). In the present study, aurone derivatives were designed and synthesized as AChE inhibitors based on the lead structure of sulfuretin. Of those synthesized, compound 10d showed ca. 1700-fold and 6-fold higher AChE inhibitory activity than sulfuretin and galantamine, respectively. This compound also ameliorated scopolamine-induced memory deficit in mice when administered orally at the dose of 1 and 2 mg/kg.
Composition for preventing or treating inflammatory bowel disease comprising benzylidene benzofuranone compound as an active ingredient
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Paragraph 0061; 0153; 0154; 0155; 0159, (2017/02/28)
The present invention relates to a composition for preventing and treating inflammatory bowel disease comprising a benzylidene benzofuranone derivative compound as an active ingredient. The benzylidene benzofuranone derivative compound is effective in maintaining the thickness of small intestine and the length of large intestine to normal states, and inhibiting inflammation with respect to large intestine, thereby being used as a pharmaceutical composition for preventing and treating inflammatory bowel disease.
Synthesis of aurones and their inhibitory effects on nitric oxide and PGE2 productions in LPS-induced RAW 264.7 cells
Shin, Seo Young,Shin, Min Cheol,Shin, Ji-Sun,Lee, Kyung-Tae,Lee, Yong Sup
experimental part, p. 4520 - 4523 (2011/09/12)
Sulfuretin is one of major constituents of Rhus verniciflua that exerts anti-inflammatory activities. Some of aurones were synthesized as sulfuretin derivatives and evaluated for their abilities to inhibit NO and PGE2 production in LPS-induced RAW 264.7 cells in order to reveal the relationship. Of the aurones synthesized in the present study, 2h and 2i, which possess C-6 hydroxyl group in A-ring and methoxy substituents in B-ring, more potently inhibited NO and PGE2 production and were less cytotoxic than sulfuretin.
Functionalized aurones as inducers of NAD(P)H:quinone oxidoreductase 1 that activate AhR/XRE and Nrf2/ARE signaling pathways: Synthesis, evaluation and SAR
Lee, Chong-Yew,Chew, Eng-Hui,Go, Mei-Lin
experimental part, p. 2957 - 2971 (2010/09/03)
The chemopreventive potential of functionalized aurones and related compounds as inducers of NAD(P)H:quinone oxidoreductase 1 (NQO1, EC 1.6.99.2) are described. Several 4,6-dimethoxy and 5-hydroxyaurones induced NQO1 activity of Hepa1c1c7 cells by 2-fold at submicromolar concentrations, making these the most potent inducers to be identified from this class. Mechanistically, induction of NQO1 was mediated by the activation of AhR/XRE and Nrf2/ARE pathways, indicating that aurones may be mixed activators of NQO1 induction or agents capable of exploiting the proposed cross-talk between the AhR and Nrf2 gene batteries. QSAR analysis by partial least squares projection to latent structures (PLS) identified size parameters, in particular those associated with non-polar surface areas, as an important determinant of induction activity. These were largely determined by the substitution on rings A and B. A stereoelectronic role for the exocyclic double bond as reflected in the E LUMO term was also identified. The electrophilicity of the double bond or its effect on the conformation of the target compound are possible key features for induction activity.
