9004-95-9Relevant academic research and scientific papers
Liposome Enhanced Detection of Amyloid Protein Aggregates
Kocsis, Istvan,Sanna, Elena,Hunter, Christopher A.
, p. 647 - 650 (2021/02/06)
Thioflavin-T is used to image amyloid aggregates because of the excellent turn-on fluorescence properties, but binding affinities are low. By mounting multiple dye units on the surface of a vesicle, the binding affinity for α-synuclein fibrils is increased by three orders of magnitude, and the optical response is increased. Cooperative interactions of the dye headgroup and lipid with the protein provide a general strategy for the construction of multivalent amyloid probes based on vesicles.
N4 - hydroxycytidine derivative as well as preparation method and application thereof
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Paragraph 0089-0093, (2021/09/01)
The invention relates to N4 - hydroxycytidine derivatives as shown in general formula I. A pharmaceutically acceptable salt, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof, and the substituted N4 - hydroxycytidine derivative structure of the structure of Formula I. The pharmaceutical composition is used for preparing medicaments for treating infections such as SARS-CoV, HBV, HCV, H1N1, Ebola and SARS-CoV - 2, can effectively inhibit influenza viruses and SARS-CoV - 2 viruses, and can have the same result on other RNA viruses. The series of compounds can be applied to preparation of anti RNA virus drugs. The medicine is used for preparing a medicine for treating virus infection and is used for preparing a vaccine adjuvant for treating virus infection.
Polycyclic pyridinone compounds and pharmaceutical compositions and uses thereof
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Paragraph 0181-0186, (2021/11/06)
The invention discloses a polycyclic pyridone compound as well as a pharmaceutical composition and application thereof, and the polycyclic pyridone compound is shown as a formula (I). The compound can be used for preparing anti-virus infection drugs.
An N4-hydroxycytoside derivative and its preparation method and use
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Paragraph 0080-0084, (2021/12/07)
The present invention provides an N4- hydroxycytidine derivative as shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof: 。 The compounds of the present invention have the following significant advantages: (1) the N4-hydroxycytidine compounds and their derivatives have a highly efficient inhibitory activity of RNA-dependent RNA polymerases of RNA viruses; (2) the N4-hydroxycytoside compounds and their derivatives and pharmaceutical compositions are widely used, can be prepared to treat / prevent SARS-CoV, HBV, HCV, H1N1, Ebola or SARS-CoV-2 virus infection disease drugs.
Preparation method of higher fatty alcohol 2-alkoxy ethanol
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Paragraph 0030; 0043; 0045-0048, (2021/08/25)
The invention provides a preparation method of higher fatty alcohol 2-alkoxy ethanol, and relates to the technical field of organic synthesis, higher fatty alcohol and sulfonyl halide are used as raw materials for cascade reaction, the higher fatty alcohol is completely converted into sulfonate under the action of alkali, and then the sulfonate is subjected to phase transfer reaction under the promotion of a phase transfer catalyst (the used phase transfer catalyst comprises quaternary ammonium salt or crown ether), sulfonate directly performs nucleophilic substitution reaction with ethylene glycol, and the reaction temperature is controlled to complete the reaction within half an hour to obtain the corresponding higher fatty alcohol 2-alkoxy ethanol. The method is low in raw material and reagent cost, simple in process operation, small in pollution, high in product yield and purity, and suitable for large-scale preparation.
Anion-Selective Cholesterol Decorated Macrocyclic Transmembrane Ion Carriers
Behera, Harekrushna,Madhavan, Nandita
, p. 12919 - 12922 (2017/09/26)
Anion transporters play a vital role in cellular processes and their dysregulation leads to a range of diseases such as cystic fibrosis, Bartter's syndrome and epilepsy. Synthetic chloride transporters are known to induce apoptosis in cancer cell lines. Herein, we report triamide macrocycles that are easily synthesized and externally functionalized by pendant membrane-permeable groups. Among a variety of chains appended onto the macrocycle scaffold, cholesterol is found to be the best with an EC50 value of 0.44 μM. The macrocycle is highly anion-selective and transports ions via an OH-/X- antiport mechanism. The macrocycle is an interesting scaffold for ion-Transport as it is able to discriminate between various anions and shows a preference for SCN- and Cl-. Such anion-selective transporters are highly attractive model systems to study ion-Transport mechanisms and could potentially be of high therapeutic value.
Containing polyoxyethylene ether hydroxy propyl aniline [...] permanaganate betaine and its preparation method
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Paragraph 0027; 0029, (2017/05/16)
The invention relates to polyoxyethylene-ether-containing hydroxypropyl anilino carboxylate betaine and a preparation method thereof, and mainly solves the problems in the prior art that an oil-displacement agent containing a surfactant is bad in oil displacement effect and high in use concentration under the oil reservoir conditions of high temperature and high salinity, and alkalis in alkali-surfactant-polymer flooding pollute and damage stratum and oil wells and severely corrode equipment and conveying pipelines. The polyoxyethylene-ether-containing hydroxypropyl anilino carboxylate betaine has the molecular general formula (I) shown in the specification, and in the formula (I), R1 is any one of C15-C39 alkyl and alkenyl, n is 1-10, R2 is any one of C1-C4 alkylidene and hydroxyl-substituted alkylidene. The technical scheme relatively well solves the problems and is applicable to tertiary oil recovery of oil fields.
Lipophilic amines as potent inhibitors of N-acylethanolamine-hydrolyzing acid amidase
Yamano, Yumiko,Tsuboi, Kazuhito,Hozaki, Yuki,Takahashi, Kiyohiro,Jin, Xing-Hua,Ueda, Natsuo,Wada, Akimori
experimental part, p. 3658 - 3665 (2012/07/28)
N-Acylethanolamines (NAEs) including N-arachidonoylethanolamine (anandamide) and N-palmitoylethanolamine are endogenous lipid mediators. These molecules are degraded to the corresponding fatty acids and ethanolamine by fatty acid amide hydrolase (FAAH) or NAE-hydrolyzing acid amidase (NAAA). Lipophilic amines, especially pentadecylamine (2c) and tridecyl 2-aminoacetate (11b), were found to exhibit potent NAAA inhibitory activities (IC50 = 5.7 and 11.8 μM), with much weaker effects on FAAH. These simple structures would provide a scaffold for further improvement in NAAA inhibitory activity.
Synthesis of fulleropyrrolidine-imidazolium salt hybrids and their solubility in various organic solvents
Itoh, Toshiyuki,Mishiro, Makoto,Matsumoto, Kei,Hayase, Shuichi,Kawatsura, Motoi,Morimoto, Minoru
, p. 1823 - 1828 (2008/09/18)
Eight types of fulleropyrrolidine-imidazolium hybrids have been synthesized and their solubility determined in various types of organic solvents. The solvent solubility of fullerene derivatives depends on the alky side chain on the imidazolium ring; modification of solvent solubility of the fulleropyrrolidine-imidazolium hybrids has thus been accomplished by introduction of an appropriate alkyl group using imidazoyl moiety as the 'functional group connector'. The imidazolium group seems to act not only as the connector but also as an important functional group that controls the solubility.
Combinatorial synthesis of PEG oligomer libraries
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Page/Page column 9, (2010/02/15)
A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
