- Rational Design of Cholesterol Derivative for Improved Stability of Paclitaxel Cationic Liposomes
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Purpose: This work explores synthesis of novel cholesterol derivative for the preparation of cationic liposomes and its interaction with Paclitaxel (PTX) within liposome membrane using molecular dynamic (MD) simulation and in-vitro studies. Methods: Chole
- Monpara, Jasmin,Kanthou, Chryso,Tozer, Gillian M.,Vavia, Pradeep R.
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- Preparation process of ethyl lauroyl arginate hydrochloride
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The invention discloses a preparation process of ethyl lauroyl arginate hydrochloride. The method comprises the following steps: 1) adding L-arginine hydrochloride into absolute ethyl alcohol, performing stirring, and dropwise adding trimethylchlorosilane to obtain L-arginine ethyl ester hydrochloride; 2) dissolving the L-arginine ethyl ester hydrochloride in absolute ethyl alcohol, and dropwise adding triethylamine and lauroyl chloride respectively to obtain an ethyl lauroyl arginate crude product; 3) mixing the ethyl lauroyl arginate crude product with deionized water and an organic solvent, removing a water phase, performing washing with saturated sodium chloride to obtain a solvent phase, and performing drying by distillation to obtain L-ethyl lauroyl arginate hydrochloride; and 4), stirring the L-ethyl lauroyl arginate hydrochloride with petroleum ether, and performing standing crystallization and suction filtration to obtain ethyl lauroyl arginate hydrochloride. The trimethylsilane is used in the preparation technological process of the ethyl lauroyl arginate hydrochloride, so that the reaction condition is mild, operation is easy, green and environment-friendly effects are achieved, the yield reaches 99% or above, and the product purity reaches 99% or above.
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Paragraph 0016-0017
(2021/10/27)
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- Method for producing ester based on eco-friendly and high efficiency esterification by using base exchange of salt and the compound thereof
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The present invention relates to an esterification reaction-based eco-friendly and high efficiency ester compound using ion exchange and an ester compound thereof. The esterification generally proceeds by reverse reaction with water, resulting in poor yield of the ester. In order to avoid hydrolysis, the esterification reaction was environmentally or non-limited due to the continuous supply of hydrochloric acid gas or the use of chlorinated thionyl chloride as a noxious substance. To the present invention, a continuous hydrochloric acid gas is provided by ion exchange of a salt, and magnesium sulfate acts as a dehydrating agent to remove water generated in esterification. In addition, the reactants are cheap and the product is also low in harmfulness and easier to handle and thus more efficient reaction is possible.
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Paragraph 0109-0115; 0117
(2021/07/07)
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- Preparation process of lauroyl arginine ethyl ester dihydrochloride
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The invention provides a preparation process of lauroyl arginine ethyl ester dihydrochloride. The preparation process comprises the following steps: (1) dissolving L-arginine monohydrochloride in ethanol to prepare arginine ethyl ester dihydrochloride; (2) dissolving lauric acid in ethyl acetate, adding carbonyl diimidazole and carrying out a reaction; (3) adding triethylamine and arginine ethyl ester dihydrochloride, and carrying out amidation to obtain a target solution; and (4) conducting cooling and crystallizing to separate out the product after washing treatment. According to the process, the carbonyl diimidazole condensing agent is used for the second-step amidation reaction, so the use of lauroyl chloride is avoided; and conditions are mild, operation is simple, and the method is green and environment-friendly. The yield of the preparation process reaches 91% or above, and product purity reaches 98% or above.
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Paragraph 0018; 0022; 0026
(2020/04/17)
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- -alkyl acyl arginine ester antibacterial agent, and preparation and application thereofN
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The invention belongs to the field of bactericides, and specifically discloses an N-alkyl acyl arginine ester antibacterial agent. The acyl group part of the N-alkyl acyl arginine esterantibacterial agent is an alkyl group with a carbon atom number of no less than 14; and the ester group part of the N-alkyl acyl arginine ester antibacterial agent is an alkyl group with a carbon atom number of no less than 2. In addition, the invention also provides a preparation method for the antibacterial agent and an application of the antibacterial agent used as a bactericide. The antibacterial agent provided by the invention is creatively discovered that the long-carbon-chain acryl group with the above-mentioned carbon atom number and the ester group with the above-mentioned carbon atom number have excellent synergistic effect and can unexpectedly and significantly shorten antibacterial time under the premise of improving antibacterial performance.
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Paragraph 0048; 0049
(2019/01/04)
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- Production and purification process of ethyl lauroyl arginate hydrochloride
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The invention discloses a production and purification process of ethyl lauroyl arginate hydrochloride. The process comprises the following steps: step A, esterfying in ethyl alcohol to obtain ethyl arginate dihydrochloride; step B, adding lauroyl chloride into ethyl arginate dihydrochloride in an organic system in the presence of organic alkali, and carrying out condensation to obtain ethyl lauroyl arginate; step C, acidifying ethyl lauroyl arginate into hydrochloride in the organic system, and purifying the product; and step D, carrying out recrystallization and precipitating solid out, and drying the solid to obtain ethyl lauroyl arginate hydrochloride. Through the production and purification process of ethyl lauroyl arginate hydrochloride, the hydrolysis of the product can be effectively avoided; the product is high in stability in industrial production; the mole yield of the product is 97% or higher; the purity of the product is 97% or higher; compared with the existing productiontechnology, the molar yield and the purity of the product are obviously improved.
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Paragraph 0036; 0046; 0050; 0052; 0058
(2018/06/26)
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- Synthesis of peptide nanofibers decorated with palladium nanoparticles and its application as an efficient catalyst for the synthesis of sulfides: Via reaction of aryl halides with thiourea or 2-mercaptobenzothiazole
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In this work supported Pd nanoparticles on a peptide nanofiber (PdNP-PNF) have been prepared via fabrication of self-assembled woven nanofiber from peptide, subsequently immobilization of palladium nanoparticles on this nanostructural compound. To obtain self-assembled woven nanofiber, we designed and synthesized a peptide using arginine as building block. The C-terminus of amino acid was protected as ethylester. Coupling was mediated by dicyclohexylecarbodiimide-1-hydroxybenzotriazole (DCC-HOBT). TEM, SEM, XRD, ICP and FT-IR techniques were employed to characterize prepared nanofiber materials. In this work, the effect of phosphate buffer solutions pH 8 and pH 11 (isoelectric point of arginine amino acid) on the structure of peptide nanofiber was investigated. Supported Pd nanoparticles on the peptide nanofiber (PdNP-PNF) were applied for the C-S coupling reaction using two different sulfur transfer reagents (thiourea and 2-mercaptobenzothiazole).
- Ghorbani-Choghamarani, Arash,Taherinia, Zahra
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p. 59410 - 59421
(2016/07/06)
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- Inhibitory effects of L-arginine derivatives on endothelium-dependent vasorelaxing response to acetylcholine of the rat aorta
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Nω-nitro-L-arginine alkyl esters (A-1-A-B) and L-arginine alkyl esters (E-1-E-B) were synthesized, and the vasorelaxing effects of acetylcholine were studied in the absence or presence of these compounds in rat aortic rings with intact endothelium that was precontracted with phenylephrine. These compounds revealed that the nitro group is an essential inhibiting group of these inhibitors, and that hydrophobic functional groups can fine-tune the binding effects. Among them, A-3 is the most potent inhibitor.
- Wang, Guei-Jane,Lai, Tzi-Chung,Chen, Chinpiao
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p. 611 - 617
(2007/10/03)
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- Process for the synthesis of cationic surfactants comprising esterification with basic character amino acids
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The process of the invention is directed to the synthesis of cationic type surfactant compounds consisting of natural basic-character amino acids, and any of their homologs, suitably modified for the purpose of obtaining products having specific applications as antimicrobial (biocidal) agents. The process comprises a first step of esterification of an amino acid, and a second step of the condensation of a fatty acid chloride with an esterified amino acid derivative. Nontoxic reaction media and catalysts are used, and a final product free from impurities is obtained. The cost of the process of the invention is reduced from prior art processes due to the use of cheaper starting materials and simpler equipment.
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