1818-27-5Relevant articles and documents
Iron-catalyzed arene C-H hydroxylation
Cheng, Lu,Wang, Huihui,Cai, Hengrui,Zhang, Jie,Gong, Xu,Han, Wei
, p. 77 - 81 (2021/10/05)
The sustainable, undirected, and selective catalytic hydroxylation of arenes remains an ongoing research challenge because of the relative inertness of aryl carbon-hydrogen bonds, the higher reactivity of the phenolic products leading to over-oxidized by-products, and the frequently insufficient regioselectivity. We report that iron coordinated by a bioinspired L-cystine-derived ligand can catalyze undirected arene carbon-hydrogen hydroxylation with hydrogen peroxide as the terminal oxidant. The reaction is distinguished by its broad substrate scope, excellent selectivity, and good yields, and it showcases compatibility with oxidation-sensitive functional groups, such as alcohols, polyphenols, aldehydes, and even a boronic acid. This method is well suited for the synthesis of polyphenols through multiple carbon-hydrogen hydroxylations, as well as the late-stage functionalization of natural products and drug molecules.
Compound for treating or preventing hepatopathy (by machine translation)
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, (2019/10/01)
The invention discloses a compound, an optical isomer or a pharmaceutically acceptable salt, an optical isomer or a pharmaceutically acceptable salt thereof for treating or preventing hepatopathy, and the compound, optical isomer or pharmaceutically acceptable salt thereof can be applied to the preparation of a medicine for treating or preventing liver diseases. (by machine translation)
2-OXO-5H-CHROMENO[4,3-B]PYRIDINES FOR USE IN THE TREATMENT OF HEPATITIS B
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Paragraph 0206, (2019/06/23)
The present invention discloses compounds according to Formula (I), wherein R1, R2a, R2b, R3, R4, and R5 are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving hepatitis B by administering the compound of the invention.
A 2, 4, 5 - trihydroxy - 3 - bromophenylmethyl synthetic method (by machine translation)
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, (2018/06/15)
The invention discloses a 2, 4, 5 - trihydroxy - 3 - bromophenylmethyl synthetic method, steps are as follows: the raw material is dissolved in tetrahydrofuran, then adding N - bromosuccinimide, add sulfuric acid reaction 48 hours to obtain the target com
Antimalarial activity of HIV-1 protease inhibitor in chromone series
Lerdsirisuk, Pradith,Maicheen, Chirattikan,Ungwitayatorn, Jiraporn
, p. 142 - 147 (2015/02/05)
Increasing parasite resistance to nearly all available antimalarial drugs becomes a serious problem to human health and necessitates the need to continue the search for new effective drugs. Recent studies have shown that clinically utilized HIV-1 protease (HIV-1 PR) inhibitors can inhibit the in vitro and in vivo growth of Plasmodium falciparum. In this study, a series of chromone derivatives possessing HIV-1 PR inhibitory activity has been tested for antimalarial activity against P. falciparum (K1 multi-drug resistant strain). Chromone 15, the potent HIV-1 PR inhibitor (IC50 = 0.65 μM), was found to be the most potent antimalarial compound with IC50 = 0.95 μM while primaquine and tafenoquine showed IC50 = 2.41 and 1.95 μM, respectively. Molecular docking study of chromone compounds against plasmepsin II, an aspartic protease enzyme important in hemoglobin degradation, revealed that chromone 15 exhibited the higher binding affinity (binding energy = -13.24 kcal/mol) than the known PM II inhibitors. Thus, HIV-1 PR inhibitor in chromone series has the potential to be a new class of antimalarial agent.
Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos
Tamura, Satoru,Yoshihira, Kunichika,Tokumaru, Mariko,Zisheng, Xu,Murakami, Nobutoshi
scheme or table, p. 3872 - 3875 (2010/08/19)
Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (FcRI), the key molecule triggering the allergic reactions, on human mast cells. As a result of analysis of structure-activity relationship of the naturally occurring and synthesized isoflavones, 7-O-methyl glycitein (11) was disclosed as the more potent inhibitor than tectorigenin (1). These isoflavone ingredients suppressed expression of FcRI more potently than the active flavonoids found previously. In addition, tectorigenin (1) was clarified to particularly reduce generation of γ-chain subunit to suppress expression of FcRI among the three subunits.
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors
Sheng, Rong,Lin, Xiao,Zhang, Jing,Chol, Kim Sun,Huang, Wenhai,Yang, Bo,He, Qiaojun,Hu, Yongzhou
experimental part, p. 6692 - 6698 (2010/01/06)
A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit ACh
2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines
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, (2008/06/13)
Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula STR1 wherein R is STR2 and R4 is STR3
