7768-28-7Relevant academic research and scientific papers
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.
Boron insertion into alkyl ether bonds via zinc/nickel tandem catalysis
Lyu, Hairong,Kevlishvili, Ilia,Yu, Xuan,Liu, Peng,Dong, Guangbin
, (2021/04/30)
Mild methods to cleave the carbon-oxygen (C?O) bond in alkyl ethers could simplify chemical syntheses through the elaboration of these robust, readily available precursors. Here we report that dibromoboranes react with alkyl ethers in the presence of a nickel catalyst and zinc reductant to insert boron into the C?O bond. Subsequent reactivity can effect oxygen-to-nitrogen substitution or one-carbon homologation of cyclic ethers and more broadly streamline preparation of bioactive compounds. Mechanistic studies reveal a cleavage-then-rebound pathway via zinc/nickel tandem catalysis.
Synthesis of high added value compounds through catalytic oxidation of 2-phenylethanol: A Kinetic study
Ben Hmida, Rania,Frikha, Nourzed,Bouguerra Neji, Soumaya,Kit, Geoffrey,Medina, Francisco,Bouaziz, Mohamed
, p. 124 - 133 (2019/12/03)
An effective procedure was developed to produce high-value added phenolic compounds through the conversion of 2-phenylethanol (2-PhEt) by using acid-activated clays KSF for the hydrogen peroxide. Owing to KSF's ability to catalyze a variety of complex oxi
Method for synthesizing darifenacin intermediate 2,3-dihydrobenzofuran
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Paragraph 0026; 0030; 0034; 0038; 0042, (2019/08/14)
The invention discloses a method for synthesizing a darifenacin intermediate 2,3-dihydrobenzofuran. The method comprises the following steps that a reaction bottle containing an organic solvent is cooled to 5-mius 5 DEG C, then a reductant and benzofuranone are added into the reaction bottle in sequence, heating is carried out for a reaction, after the reaction is completed, a reaction solution iscooled, the cooled reaction solution is quenched, concentrated, extracted, dried and filtered, and a filtrate is concentrated to obtain 2-hydroxyphenethylethanol; the 2-hydroxyphenylethanol and an acidic catalyst are added into the organic solvent, a reaction is performed under a heating condition, after the reaction is completed, a reaction solution is cooled, water is added into the cooled reaction solution, mixing and uniform stirring are carried out, standing and separating are carried out, an organic phase is dried and filtered, and reduced pressure distillation is performed to obtain the darifenacin intermediate 2,3-dihydrobenzofuran. The method for synthesizing the darifenacin intermediate 2,3-dihydrobenzofuran has the advantages that the synthetic method is simpler, the reaction condition is mild, the yield is high, the purity is high, and the cost is low.
Two new aromatic glycosides, elengiosides A and B, from the flowers of Mimusops elengi
Morikawa, Toshio,Manse, Yoshiaki,Koda, Mika,Chaipech, Saowanee,Pongpiriyadacha, Yutana,Muraoka, Osamu,Ninomiya, Kiyofumi
, p. 542 - 550 (2017/12/26)
Two new aromatic glycosides, elengiosides A (1) and B (2), were isolated from the methanolic extract of the flowers of Mimusops elengi (Sapotaceae) together with 26 known compounds. Their stereostructures were elucidated based on their spectroscopic properties and chemical evidence. Among the isolates, a phenylethanoid glycoside, undatuside C (14), was found to exhibit hyaluronidase inhibitory activity.
PHENOLATE TRANSITION METAL COMPLEXES, PRODUCTION AND USE THEREOF
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Page/Page column 30; 31, (2018/02/28)
Phenolate ligands and transition metal complexes are disclosed for use in alkene polymerization, with optional chain transfer agent, to produce polyolefins.
Cyclic ether synthesis from diols using trimethyl phosphate
Asai, Shota,Kato, Maho,Monguchi, Yasunari,Sajiki, Hironao,Sawama, Yoshinari
supporting information, p. 4787 - 4790 (2017/07/06)
Cyclic ethers have been effectively synthesized via the intramolecular cyclization of diols using trimethyl phosphate and NaH. The present cyclization could proceed at room temperature to produce 5-7 membered cyclic ethers in good to excellent yields. Substrates possessing a chiral secondary hydroxy group were transformed into the corresponding chiral cyclic ethers along with the retention of their stereochemistries.
Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety
Xie, Jin,Yang, Fengzhi,Zhang, Man,Lam, Celine,Qiao, Yixue,Xiao, Jia,Zhang, Dongdong,Ge, Yuxuan,Fu, Lei,Xie, Dongsheng
, p. 131 - 134 (2016/12/27)
A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2′-position of phenylethanol moiety could significantly enhance CAPE's antiproliferative activity. 2′-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50?=?0.4?±?0.02 & 0.6?±?0.03?μM against Hela and DU-145 respectively).
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Page/Page column 60; 61, (2014/10/15)
The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Page/Page column 38; 39, (2014/10/18)
The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. Formule (I)
