36603-49-3Relevant articles and documents
Discovery of Salidroside-Derivated Glycoside Analogues as Novel Angiogenesis Agents to Treat Diabetic Hind Limb Ischemia
Han, Jingxuan,He, Yun,Huang, Song,Kasim, Vivi,Liu, Caiping,Marcelina, Olivia,Miyagishi, Makoto,Nugrahaningrum, Dyah Ari,Wang, Guixue,Wu, Shourong,Zou, Meijuan
supporting information, (2022/01/14)
Therapeutic angiogenesis is a potential therapeutic strategy for hind limb ischemia (HLI); however, currently, there are no small-molecule drugs capable of inducing it at the clinical level. Activating the hypoxia-inducible factor-1 (HIF-1) pathway in skeletal muscle induces the secretion of angiogenic factors and thus is an attractive therapeutic angiogenesis strategy. Using salidroside, a natural glycosidic compound as a lead, we performed a structure-activity relationship (SAR) study for developing a more effective and druggable angiogenesis agent. We found a novel glycoside scaffold compound (C-30) with better efficacy than salidroside in enhancing the accumulation of the HIF-1α protein and stimulating the paracrine functions of skeletal muscle cells. This in turn significantly increased the angiogenic potential of vascular endothelial and smooth muscle cells and, subsequently, induced the formation of mature, functional blood vessels in diabetic and nondiabetic HLI mice. Together, this study offers a novel, promising small-molecule-based therapeutic strategy for treating HLI.
Preparation method of 4-(4-hydroxyphenyl) cyclohexanone
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Paragraph 0078-0081, (2019/08/01)
The invention relates to the technical field of chemical synthesis, in particular to a preparation method of 4-(4-hydroxyphenyl) cyclohexanone. According to the preparation method, p-bromophenol is used as a raw material, a Grignard reagent is prepared through hydroxyl protection and Grignard reaction, then the prepared Grignard reagent is utilized to couple with 1,4-cyclohexanedione monoethyleneglycol ketal, then the product is dehydrated to obtain alkene, and double protecting groups are removed after hydrogenation to prepare a target product, namely, 4-(4-hydroxyphenyl) cyclohexanone. Thepreparation method of 4-(4-hydroxyphenyl) cyclohexanone, provided by the invention, has the advantages of reasonable process design, high yield and low production cost; the prepared 4-(4-hydroxyphenyl) cyclohexanone is a white solid, the HPLC content is more than 99.5%, the total yield of the product can reach 75-80%, and the raw materials are easy to obtain; and the method has simple operation and high safety, and realizes industrial production of 4-(4-hydroxyphenyl) cyclohexanone.
Phosphoramidate prodrug of nucleoside analogues, a pharmaceutical composition and applications of the phosphoramidate prodrug
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Paragraph 0146-0148; 0161-0163; 0202-0204; 0207-0209, (2019/04/10)
The invention relates to phosphoramidate prodrug of nucleoside analogues, or stereoisomers of the phosphoramidate prodrug, or a mixture of the stereoisomers of the phosphoramidate prodrug, or pharmaceutically acceptable salts or solvates of the phosphoramidate prodrug, and applications in the preparation of medicine for preventing or treating hepatitis B virus (HBV) and/or human immunodeficiency virus (HIV) infection alone or in combination with other medicine. The anti-HBV activity of the compound of the invention is equivalent to that of tenofovir alafenamide fumarate (TAF), and the compoundof the invention has the anti-liver fibrosis effect, can help improve the therapeutic effect of patients, and has good safety important clinical significance.