10226-29-6Relevant articles and documents
A direct retro-Barbier fragmentation
Zhang, Wen-Chun,Li, Chao-Jun
, p. 5831 - 5833 (2000)
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A novel galantamine-curcumin hybrid as a potential multi-target agent against neurodegenerative disorders
Atanasova, Mariyana,Doytchinova, Irini,Philipova, Irena,Simeonova, Rumyana,Stavrakov, Georgi,Valkova, Iva,Zheleva, Dimitrina
, (2021)
The acetylcholinesterase (AChE) inhibitors are the main drugs for symptomatic treatment of neurodegenerative disorders like Alzheimer’s disease. A recently designed, synthesized and tested hybrid compound between the AChE inhibitor galantamine (GAL) and the antioxidant polyphenol curcumin (CU) showed high AChE inhibition in vitro. Here, we describe tests for acute and shortterm toxicity in mice as well as antioxidant tests on brain homogenates measured the levels of malondialdehide (MDA) and glutathione (GSH) and in vitro DPPH, ABTS, FRAP and LPO inhibition assays. Hematological and serum biochemical analyses were also performed. In the acute toxicity tests, the novel AChE inhibitor given orally in mice showed LD50 of 49 mg/kg. The short-term administration of 2.5 and 5 mg/kg did not show toxicity. In the ex vivo tests, the GAL-CU hybrid performed better than GAL and CU themselves; in a dose of 5 mg/kg, it demonstrates 25% reduction in AChE activity, as well as a 28% and 73% increase in the levels of MDA and GSH, respectively. No significant changes in blood biochemical data were observed. The antioxidant activity of 4b measured ex vivo was proven in the in vitro tests. In the ABTS assay, 4b showed radical scavenging activity 10 times higher than the positive control butylhydroxy toluol (BHT). The GAL-CU hybrid is a novel non-toxic AChE inhibitor with high antioxidant activity which makes it a prospective multitarget drug candidate for treatment of neurodegenerative disorders.
Bellas et al.
, p. 5149,5152 (1969)
Ring-opening iodination and bromination of unstrained cycloalkanols through ?-scission of alkoxy radicals
Shi, Jiang-Ling,Wang, Yuankai,Wang, Zixuan,Dou, Bowen,Wang, Jianbo
supporting information, p. 5002 - 5005 (2020/05/18)
Ring-opening iodination or bromination of unstrained cycloalkanols with NaI or NaBr and PhI(OAc)2 under visible light irradiation is developed. In this protocol the concentration of I2is modulated through the generation of triiodide (I3-), thus significantly avoiding undesired side reactions. The reaction is under mild conditions and has a wide substrate scope, thus providing a practically useful method for accessing ω-iodo or ω-bromoketones.