Category: indole-building-block. Authors Simeonova, R; Zheleva, D; Valkova, I; Stavrakov, G; Philipova, I; Atanasova, M; Doytchinova, I in MDPI published article about in [Simeonova, Rumyana; Zheleva, Dimitrina; Valkova, Iva; Stavrakov, Georgi; Atanasova, Mariyana; Doytchinova, Irini] Med Univ Sofia, Fac Pharm, Sofia 1000, Bulgaria; [Stavrakov, Georgi; Philipova, Irena] Bulgarian Acad Sci, Inst Organ Chem, Ctr Phytochem, Sofia 1113, Bulgaria in 2021, Cited 61. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
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 short-term 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.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles