39927-08-7Relevant academic research and scientific papers
Effective Na+-Binding Ability and Molecular Assembly of an Alkylamide-Substituted Penta(ethylene)glycol Derivative
Seto, Shinya,Takeda, Takashi,Hoshino, Norihisa,Akutagawa, Tomoyuki
, p. 6349 - 6358 (2021)
A new amphiphilic penta(ethylene glycol) derivative (1) bearing two hydrogen-bonding -CONHC14H29 chains was prepared. Compound 1 exhibited ion-recognition abilities for Na+ and K+, and its properties were compared with those of the macrocyclic [18]crown-6. Although both compound 1 and [18]crown-6 have six ether oxygen atoms (-OC2H2-), the Na+-binding ability of the former was much higher than that of the latter. K+-binding ability of cyclic [18]crown-6 was much higher than its Na+-binding ability, while the reverse was true for acyclic compound 1. Single-crystal X-ray structural analysis of Na+·1·B(Ph)4-·(hexane)2 at 100 K revealed the existence of a wrapped Na+-coordination by six ether and one carbonyl oxygen atoms of 1, which was further stabilized by intramolecular N-H···O= hydrogen-bonding interactions. The complex phase transition during glass (G) formation and recrystallization was confirmed in the thermal cycle of Na+·1·B(Ph)4-, whose molten state showed two kinds of liquid phases, Na+-complexed (Na+·1) + B(Ph)4- and completely dissociated Na+ + 1 + B(Ph)4-. The Na+ conductivity of the molten state was 2 orders of magnitude higher than that of the G phase.
GPER PROTEOLYTIC TARGETING CHIMERAS
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, (2021/10/30)
A molecule comprising a G-protein coupled estrogen receptor (GPER) ligand coupled to a linker coupled to an E3 ubiquitin ligase ligand and methods of using the molecule are provided. In one embodiment, the GPER ligand is estradiol and the E3 ubiquitin lig
BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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, (2019/06/19)
It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
IRAK DEGRADERS AND USES THEREOF
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, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
SMALL MOLECULES
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, (2018/11/10)
Compounds having the general structure A - L - B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1 B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.
Homo-PROTACs: Bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
Maniaci, Chiara,Hughes, Scott J.,Testa, Andrea,Chen, Wenzhang,Lamont, Douglas J.,Rocha, Sonia,Alessi, Dario R.,Romeo, Roberto,Ciulli, Alessio
, (2017/10/16)
E3 ubiquitin ligases are key enzymes within the ubiquitin proteasome system which catalyze the ubiquitination of proteins, targeting them for proteasomal degradation. E3 ligases are gaining importance as targets to small molecules, both for direct inhibition and to be hijacked to induce the degradation of non-native neo-substrates using bivalent compounds known as PROTACs (for 'proteolysis-targeting chimeras'). We describe Homo-PROTACs as an approach to dimerize an E3 ligase to trigger its suicide-type chemical knockdown inside cells. We provide proof-of-concept of Homo-PROTACs using diverse molecules composed of two instances of a ligand for the von Hippel-Lindau (VHL) E3 ligase. The most active compound, CM11, dimerizes VHL with high avidity in vitro and induces potent, rapid and proteasome-dependent self-degradation of VHL in different cell lines, in a highly isoform-selective fashion and without triggering a hypoxic response. This approach offers a novel chemical probe for selective VHL knockdown, and demonstrates the potential for a new modality of chemical intervention on E3 ligases.
Ether acid cobalt complex single crystal and preparation method as well as application thereof
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Paragraph 0018; 0019, (2016/12/01)
The invention discloses ether acid cobalt complex single crystal, having a structure of [Co(L)(H2O)], wherein L is equal to di-ethoxy di-acetic acid. The invention also discloses a preparation method of the single crystal. According to the preparation method, a normal temperature volatilization method is adopted, i.e., L and Co(Ac)2.H2O are stirred in water for half an hour, and then are filtered, and filtrate is volatilized at normal temperature for two weeks, thus obtaining red blocky crystal suitable for X-ray single crystal diffraction, wherein the mol ratio of Co(Ac)2.H2O is 1 to 1. The invention further discloses application of the ether acid cobalt complex single crystal as a potential fluorescent material in detection on the adsorption quantity of a dye or an illuminating agent.
Reactions of peroxide products of ozonolysis of allyl ethers/esters in the AcOH-CH2Cl2 system on treatment with semicarbazide hydrochloride
Raskil'dina, Gulnara Z.,Legostaeva, Yuliya V.,Garifullina, Liliya R.,Sultanova, Rimma M.,Ishmuratov, Gumer Y.,Zlotskii, Simon S.
, p. 652 - 656 (2017/01/13)
Background: A one-pot method for the preparation of the corresponding alkoxy acetic acids by low-temperature ozonolysis of allyl ethers/esters followed by treatment with semicarbazide hydrochloride has been suggested. The reaction occurs via formation of acetoxyhydroperoxide, subsequent reduction of which depends on the process temperature and the nature of the starting substrate. Objective: The article is aimed at the development of one-pot method for obtaining practically important alkoxy acetic acids, because the ozonolytic cleavage of a ?=? double bond is the key step in full syntheses of many biologically active compounds. Methods: We used a low temperature ozonolysis of functionally substituted olefins in the system acetic acid-methylene dichloride followed by reduction of semicarbazide hydrochloride. To create a method we have used available allyl ethers/esters as starting materials. Results: We investigated reaction of the peroxide products of ozonolysis of monoallyl ethers, ester and diallyl ethers in an AcOH/CH2Cl2 mixture on treatment with semicarbazide hydrochloride at various temperatures. We have discovered that the selectivity of reduction of acetoxyhydroperoxide formed at the first stage depends both on the process temperature and on the nature of the starting substrate. A decrease in temperature favors acid hydrolysis and formation of a carboxylic acid. Conclusion: We have proposed a simple and highly efficient one-pot method for the preparation alkoxy acetic acids without isolation of intermediate peroxides.
Ether acid copper complex monocrystal, and preparation method and application thereof
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Paragraph 0018; 0019, (2016/10/10)
The invention discloses an ether acid copper complex monocrystal. The structure of the monocrystal is [Cu(L)(H2O)2], wherein L is ethyldioxydiacetic acid. The invention also discloses a preparation method of the monocrystal. The method adopts a normal temperature volatilization technology, and concretely comprises the following steps: stirring the L and Cu(Ac)2.H2O in water for 0.5h, filtering the obtained solution, and volatilizing the obtained filtrate at normal temperature for 2 weeks in order to obtain the blue block crystal suitable for X-ray single crystal diffraction, wherein a molar ratio of the L to Cu(Ac)2.H2O is 1:1. The invention further discloses an application of the ether acid copper complex monocrystal in detection of the adsorption quantity of a dye or a luminescence agent as a potential fluorescent material.
Selective recovery of rare earth elements using chelating ligands grafted on mesoporous surfaces
Florek, Justyna,Mushtaq, Ambreen,Larivière, Dominic,Cantin, Gabrielle,Fontaine, Frédéric-Georges,Kleitz, Freddy
, p. 103782 - 103789 (2015/12/24)
Nowadays, rare earth elements (REEs) and their compounds are critical for the rapidly growing advanced technology sectors and clean energy demands. However, their separation and purification still remain challenging. Among different extracting agents used for REE separation, the diglycolamide (DGA)-based materials have attracted increasing attention as one of the most effective extracting agents. In this contribution, a series of new and element-selective sorbents were generated through derivatisation of the diglycolamide ligand (DGA), grafted to mesoporous silica and tested for the separation of rare earth elements. It is shown that, by tuning the ligand bite angle and its environment, it is possible to improve the selectivity towards specific rare earth elements.
