- Nanostructure formation in aqueous solution of amphiphilic copolymers of 2-(N,N-dimethylaminoethyl)methacrylate and alkylacrylate: Characterization, antimicrobial activity, DNA binding, and cytotoxicity studies
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Three amphiphilic random copolymers poly(2-(dimethylaminoethyl) methacrylate-co-alkylacrylate) (where, alkyl = hexyl, octyl, dodecyl) with 16 mol% hydrophobic substitution were synthesized. Surface tension, viscosity, fluorescence probe, dynamic light scattering (DLS), as well as transmission electron microscopic (TEM) techniques were utilized to investigate self-assembly formation by the hydrophobically modified polymers (HMPs) in pH 5. Formation of hydrophobic domains through inter-polymer chain interaction of the copolymer in dilute solution was confirmed by fluorescence probe studies. Average hydrodynamic diameter of the copolymer aggregates at different polymer concentration was measured by DLS studies. The copolymer with shorter hydrophobic chain exhibits larger hydrodynamic diameter in dilute solution, which decreased with either increase of concentration or increase of hydrophobic chain length. TEM images of the dilute solutions of the copolymers with shorter as well as with longer hydrophobic chain exhibit spherical aggregates of different sizes. The antimicrobial activity of the copolymers was evaluated by measuring the minimum inhibitory concentration value against one Gram-positive bacterium Bacillus subtilis and one Gram-negative bacterium Escherichia coli. The copolymer with the octyl group as pendent hydrophobic chain was found to be more effective in killing these microorganisms. The interaction of the cationic copolymers with calf-thymus DNA was studied by fluorescence quenching method. The polymer-DNA binding was found to be purely electrostatic in nature. The hydrophobes on the polymer backbone were found to have a significant influence on the binding process. Biocompatibility studies of the copolymers in terms of cytotoxicity measurements were finally performed at different concentrations of the HMPs to evaluate their potential application in biomedical fields.
- Dutta, Pranabesh,Dey, Joykrishna,Shome, Anshupriya,Das, Prasanta Kumar
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- Novel dihydroisoxazoline-alkyl carbon chain hybrid artemisinin analogues (artemalogs): Synthesis and antitumor activities
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Two new series of dihydroisoxazoline-alkyl carbon chain hybrid artemisinin analogues (artemalogs) were designed and synthesized though a 1,3-dipolar cycloaddition. Subsequent pharmacological screening led to several compounds having dramatically improved antiproliferative effects against several human tumor cell lines compared to artemisinin and dihydroartemisinin. Mechanistic studies on the most potent artemalogs were investigated.
- Liu, Gang,Song, Shanshan,Liu, Xiaohua,Zhang, Ao,Miao, Zehong,Ding, Chunyong
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- Preparation process of long-chain alkyl (meth) acrylate
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The invention discloses a preparation process of long-chain alkyl (meth) acrylate, which adopts a polymerization inhibitor composition containing phenothiazine accounting for at least 10% of the totalmass of the composition as a polymerization inhibitor for esterification reaction. The invention solves the problem of self-polymerization in the post-treatment process, can effectively control the acidity of the product to obtain a colorless or white high-purity product, and has the advantages of high yield and expanded application range of the product; in addition, according to the preparationprocess, polymerized excessive (methyl) acrylic acid is recycled, so that a large amount of acid wastewater is prevented from being generated, and the comprehensive benefit is increased.
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Paragraph 0041; 0042
(2021/01/12)
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- Efficient metal-containing cationic antitumor drug as well as preparation method and application thereof
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The invention relates to a metal-containing efficient cationic antitumor drug as well as a preparation method and an application thereof. Specifically, the invention relates to metal cationic compounds of formula I wherein M is a divalent metal, n is an integer from 1 to 10, X is independently selected from O, S and NH, and R is a hydrophobic chain hydrocarbyl group. The metal cation medicine disclosed by the invention has broad-spectrum anticancer property, does not generate drug resistance, reduces toxic and side effects while improving the anti-tumor effect, and can be used for treating tumors without a carrier. In addition, the amphiphilic micromolecule structure is simple, can play a role without entering cells, does not generate drug resistance, and can inhibit tumor metastasis.
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Paragraph 0053-0054
(2021/06/26)
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- Ruthenium(II) Catalysed Highly Regioselective C-3 Alkenylation of Indolizines and Pyrrolo[1,2-a]quinolines
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Discovered the Ruthenium(II) catalysed highly stereo- and regioselective protocol for the oxidative C-3 alkenylation of indolizines and pyrrolo[1,2-a]quinolines. The methodology represents the first example for the directing group assisted C–C bond formation reaction of the indolizines. Under mild reaction conditions, this method provides an ample substrate scope to produce C-3 alkenyl indolizines in excellent to moderate yields. However, pyrrolo[1,2-a]quinolines underwent alkenynation at elevated temperature to furnish C-3 alkenyl derivatives. The functionalized indolizines were selectively reduced to obtain their saturated derivatives.
- Jadhav, Pankaj Pandit,Kahar, Nilesh Machhindra,Dawande, Sudam Ganpat
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supporting information
p. 7831 - 7835
(2019/12/24)
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- Direct Deuteration of Acrylic and Methacrylic Acid Derivatives Catalyzed by Platinum on Carbon in Deuterium Oxide
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The platinum on carbon (Pt/C)-catalyzed deuteration of acrylic and methacrylic acid derivatives in deuterium oxide (D2O) efficiently proceeded to give the corresponding acrylic acid-d3 and methacrylic acid-d5 derivatives. The olefinic functionality, as well as the methyl group on the unsaturated functionality of the substrate, were satisfactorily deuterated via the hydrogen (H)-deuterium (D) exchange reaction. The obtained deuterated compounds are useful building blocks and efficiently converted to the corresponding desired products including a polymer without the degradation of the original deuterium contents. (Figure presented.).
- Park, Kwihwan,Matsuda, Takumi,Yamada, Tsuyoshi,Monguchi, Yasunari,Sawama, Yuka,Doi, Naoki,Sasai, Yasushi,Kondo, Shin-Ichi,Sawama, Yoshinari,Sajiki, Hironao
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supporting information
p. 2303 - 2307
(2018/05/07)
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- Highly-functionalized arene synthesis based on palladium on carbon-catalyzed aqueous dehydrogenation of cyclohexadienes and cyclohexenes
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Transition metal-catalyzed dehydrogenation is a clean oxidation method requiring no additional oxidants. We have accomplished a heterogeneous Pd/C-catalyzed aqueous dehydrogenation of 1,4-cyclohexadienes and cyclohexenes to give the corresponding highly-functionalized arenes. Furthermore, various arenes could be efficiently constructed in a one-pot manner via a Diels-Alder reaction and the following dehydrogenation.
- Yasukawa, Naoki,Yokoyama, Hiroki,Masuda, Masahiro,Monguchi, Yasunari,Sajiki, Hironao,Sawama, Yoshinari
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supporting information
p. 1213 - 1217
(2018/03/28)
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- Preparation method for synthesizing high-carbon alkyl acrylate through catalyzing in-situ acid resin
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The invention belongs to the technical field of organic synthesis and in particular relates to a preparation method for synthesizing high-carbon alkyl acrylate through catalyzing in-situ acid resin. The preparation method comprises the following steps: mixing acrylic acid, the in-situ acid resin, acrylic high-carbon alkyl alcohol, hydroquinone and cyclohexane according to a certain ratio; stirringand heating, and controlling reaction time; after reaction is finished, filtering to remove a resin catalyst; carrying out water washing, neutralization and water washing to obtain the high-carbon alkyl acrylate. According the preparation method provided by the invention, the yield of high-carbon alkyl acrylate can be improved; the in-situ acid resin can be repeatedly utilized, resources are saved and the environment is protected.
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Paragraph 0037; 0038
(2018/11/27)
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- Broadly Applicable Ytterbium-Catalyzed Esterification, Hydrolysis, and Amidation of Imides
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An efficient, broadly applicable, operationally simple, and divergent process for the transformation of imides into a range of carboxylic acid derivatives under mild conditions is reported. By simply using catalytic amounts of ytterbium(III) triflate as a Lewis acid promoter in the presence of alcohols, water, amines, or N,O-dimethylhydroxylamine, a broad range of imides is smoothly and readily converted to the corresponding esters, carboxylic acids, amides, and Weinreb amides in good yields. This method notably enables an easy cleavage of oxazolidinone-based auxiliaries.
- Guissart, Céline,Barros, Andre,Rosa Barata, Luis,Evano, Gwilherm
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supporting information
p. 5098 - 5102
(2018/09/13)
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- Lipid modified spermine derivatives and the use of the derivatives of the prepared liposome
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The invention provides a liposome-modified spermine derivative and a liposome prepared by the derivative. The spermine derivative is directly applied or is mixed with one or more selected from cholesterol, neutral lipids and polyethylene glycol (PEG)-modified lipids, which can be adopted as a carrier for entrapping or absorbing bioactive molecular drugs to be loaded into cells. In this way, the effect of regulation, intervention or treatment is realized. In a general formula (1), X1 represents -(CH2)- or carbonyl group, wherein n represents 1, 2 or 3; X2 represents -(CH2)-, ester group, amide group, oxygen, or sulfur; R1 and R2 independently represent C6-C18 alkyl group or lipophilic cholesterol molecules, respectively.
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Paragraph 0126-0128; 0131-0132
(2017/08/25)
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- Synthesis and Surface Properties of a Novel Sodium 3-(3-Alkyloxy-3-oxopropoxy)-3-oxopropane-1-sulfonate at the Air-Water Interface
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The present paper describes the synthesis and evaluation of surface properties of a novel series of anionic surfactant, namely sodium 3-(3-alkyloxy-3-oxopropoxy)-3-oxopropane-1-sulfonate with varying alkyl chain length (C8-C16). Synthesis involves initial formation of the 3-alkyloxy-3-oxopropyl acrylate along with fatty acrylate during the direct esterification of fatty alcohol with acrylic acid in the presence of 0.5 % NaHSO4 at 110 C followed by sulfonation of the terminal double bond of the 3-alkyloxy-3-oxopropyl acrylate. Synthesized compounds were evaluated for surface and thermodynamic properties such as critical micelle concentration (CMC), surface tension at CMC (γcmc), efficiency of surface adsorption (pC20), surface excess (Γmax), minimum area per molecule at the air-water interface (A min), free energy of adsorption (?G ads), free energy of micellization (?G mic), wetting time, emulsifying properties, foaming power and calcium tolerance. Effect of chain length on CMC follows the classic trend, i.e. decrease in CMC with the increase in alkyl chain length. High pC20 (>3) value indicates higher hydrophobic character of the surfactant. These surfactants showed very poor wetting time and calcium tolerance, but exhibited good emulsion stability and excellent foamability. Foaming power and foam stability of C14-sulfonate were found to be the best among the studied compounds. Foam stability of C14-sulfonate was also studied at different concentrations over time and excellent foam stability was obtained at a concentration of 0.075 %. Thus this novel class of surfactant may find applications as foam boosters in combination with other suitable surfactants.
- Kumar, Pandari Phani,Nayak, Rati Ranjan,Kanjilal, Sanjit
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p. 689 - 695
(2015/06/23)
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- Cosmetic emulsions containing acrylamide copolymer
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Water-in-oil emulsions wherein the emulsifier is a copolymer of 1 mol of acrylamide with 2 to 20 mols of at least one ethylenically unsaturated ester copolymerizable therewith selected from the group consisting of vinyl alkylcarboxylates, alkyl and cycloalkyl acrylates, and alkly and cycloalkyl methacrylates, wherein the alkyl and cycloalkyl groups contain 6 to 24 carbon atoms, and the continuous phase is a cosmetically acceptable oil, which can be prepared easily, safely and inexpensively. The emulsions are substantially odorless and are cosmetically acceptable for the care of the skin.
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