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N-Peptidyl-D-glucosamines were synthesized by the stepwise reaction of N-carboxy alpha -amino acid anhydrides (4-alkyl-2,5-oxazolidinediones) with D-glucosamine hydrochloride in the presence of equimolar sodium methoxide in a mixture of acetonitrile and methanol, or in methanol, at a low temperature. Polymerization reaction of N-carboxy alpha -amino acid anhydrides (NCAs) did not occur at minus 50 degree C. The mechanism of the reaction was then studied.

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The invention relates to a kind of the acid is sensitive of amphiphilic triblock polymer, the polymer is composed of polyethylene glycol – acid sensitive section 1 – acid sensitive section 2 triblock copolymer, the states the acid sensitive section 1 is polyacrylamide benzene boronic acid, the states the acid sensitive section 2 is dimethyl ethylenediamine gathers the ammonia acid radical, said polyethylene glycol has a molecular weight of 2000 – 5000, the states the acid sensitive section 1 has a molecular weight of 2000 – 6000, the states the acid sensitive section 2 has a molecular weight of 1000 – 2000. The invention also involves the above-mentioned the acid is sensitive of amphiphilic triblock polymer for the preparation of a pharmaceutical and co-transmission liquid fluorocarbon polymer nano vesicle in the application, the nanometer vesicle has uniform nanometer diameter, can be stable in vivo circulation and enriched in tumor site; nano-vesicle of the present invention also has good enhanced ultrasound developing ability thus in diagnostic ultrasound under the conditions of the ultrasonic imaging application, the polymer nano-vesicle also having ultrasonic sensitivity, in the low frequency high energy ultrasonic irradiation of excitation cavitation effect under the condition of, to achieve controlled release of the medicament. (by machine translation)

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Reference:
Oxazolidine – Wikipedia,
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Dendritic polymers represent a class of materials for prospective drug delivery application. For that purpose we present the synthesis and characterization of hydrophilic, anionic core-shell architectures based on poly(ethylene imine) (PEI) as core molecule and polyamino acid chains (composed of glutamic acid or aspartic acid) as shell component. NCA polymerization is used for coupling polyamino acid chains to PEI scaffold. Modifying these structures with sugar molecules result in the formation of new core-shell architectures combining a mixture of binary and double shell. For their potential biomedical applications the solution properties of these anionic core-shell architectures at various pH values (3-9) were studied by different analytical tools (zeta potential, streaming potential pH titration, DLS, AFM, in-situ AFM, TEM and cryo-TEM). Especially, the sugar-decorated core-shell architectures mainly provide isolated macromolecules over a broad pH range. Furthermore, the anionic core-shell architectures are suited to interact with cationic molecules.

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Hetero- and homopolymers prepared from alpha-amino acid-N-carboxyanhydrides (NCAs) monomers are widely useful products. The preparation of pure NCA monomers has been extensively studied in the past. Purification methods including repeated crystallizations, extraction, and flash column chromatography have been devised. However, these methods are not easily amendable to large-scale NCA preparations. This article describes the synthesis of numerous highly purified NCAs on a >100 g scale using a simple filtration step through diatomaceous earth (celite). The resulting NCAs provided polyethylene glycol (PEG)?amino acid triblock polymers devoid of low-molecular-weight by-products that were routinely observed when unfiltered batches of NCAs were used. Also disclosed is the preparation of NCAs at ambient temperature. Traditionally, NCA reactions using a phosgene source are heated. This study shows these reactions can be driven by the slight exotherm that forms upon reagent mixing. This eliminates the need for an external heating source, simplifying large-scale reactions.

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Oxazolidine – Wikipedia,
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A new entity of polymer vesicle with a polyion complex (PIC) membrane, a PICsome, was prepared by simple mixing of a pair of oppositely charged block copolymers, composed of biocompatible PEG and poly(amino acid)s, in an aqueous medium. Flow particle image analysis revealed the formation of spherical particles with a size range up to 10 mum. Observation by dark-field and confocal laser scanning microscopes clearly confirmed that the PICsome has a hollow structure with an inner-water phase, in which FITC-dextran emitting green fluorescence was successfully encapsulated simply by the simultaneous mixing with the block copolymers. Confocal laser scanning microscopic observation and spectral analysis revealed the smooth penetration of a low molecular weight fluorescent dye (TRITC; MW = 443.5) emitting red fluorescence into the FITC-dextran encapsulated PICsome to give the PICsome image with a merged color of yellows, indicating the semipermeable nature of the PICsome membrane. The PICsomes showed appreciable physiological stability even in the presence of serum proteins, suggesting their feasibility in biomedical fields such as carriers of therapeutic compounds and compartments for diagnostic enzymes. Copyright

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Purpose: To identify the effects of cross-linkers and drug-binding linkers on physicochemical and biological properties of polymer nanoassembly drug carriers. Methods: Four types of polymer nanoassemblies were synthesized from poly(ethylene glycol)-poly(aspartate) [PEG-p(Asp)] block copolymers: self-assembled nanoassemblies (SNAs) and cross-linked nanoassemblies (CNAs) to each of which an anticancer drug doxorubicin (DOX) was loaded by either physical entrapment or chemical conjugation (through acid-sensitive hydrazone linkers). Results: Drug loading in nanoassemblies was 27 ~ 56% by weight. The particle size of SNA changed after drug and drug-binding linker entrapment (20 ~ 100 nm), whereas CNAs remained 30 ~ 40 nm. Drug release rates were fine-tunable by using amide cross-linkers and hydrazone drug-binding linkers in combination. In vitro cytotoxicity assays using a human lung cancer A549 cell line revealed that DOX-loaded nanoassemblies were equally potent as free DOX with a wide range of drug release half-life (t1/2 = 3.24 ~ 18.48 h, at pH 5.0), but 5 times less effective when t1/2 = 44.52 h. Conclusion: Nanoassemblies that incorporate cross-linkers and drug-binding linkers in combination have pharmaceutical advantages such as uniform particle size, physicochemical stability, fine-tunable drug release rates, and maximum cytotoxicity of entrapped drug payloads.

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The invention relates to a kind of the acid is sensitive of amphiphilic triblock polymer, the polymer is composed of polyethylene glycol – acid sensitive section 1 – acid sensitive section 2 triblock copolymer, the states the acid sensitive section 1 is polyacrylamide benzene boronic acid, the states the acid sensitive section 2 is dimethyl ethylenediamine gathers the ammonia acid radical, said polyethylene glycol has a molecular weight of 2000 – 5000, the states the acid sensitive section 1 has a molecular weight of 2000 – 6000, the states the acid sensitive section 2 has a molecular weight of 1000 – 2000. The invention also involves the above-mentioned the acid is sensitive of amphiphilic triblock polymer for the preparation of a pharmaceutical and co-transmission liquid fluorocarbon polymer nano vesicle in the application, the nanometer vesicle has uniform nanometer diameter, can be stable in vivo circulation and enriched in tumor site; nano-vesicle of the present invention also has good enhanced ultrasound developing ability thus in diagnostic ultrasound under the conditions of the ultrasonic imaging application, the polymer nano-vesicle also having ultrasonic sensitivity, in the low frequency high energy ultrasonic irradiation of excitation cavitation effect under the condition of, to achieve controlled release of the medicament. (by machine translation)

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The present invention refers to nano anticancer number thereof relates to number bath method. More specifically, the present invention refers to hydrophobic anti-cancer drugs, pH sensitive peptide, including nano – and Poloxamer folate conjugates anticancer number type, and the following formula 1. number bath method. (by machine translation)

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Safety of (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 13590-42-6, name is (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate. In an article,Which mentioned a new discovery about 13590-42-6

Purpose: To develop block copolymer micelles as an aqueous dosage form for a potent glycolytic enzyme inhibitor, 3-(3- pyridinyl)-1-(4-pyridinyl)-2-propen- 1-one (3PO). Methods: The micelles were prepared from poly(ethylene glycol)-poly(aspartate hydrazide) [PEG-p(HYD)] block copolymers to which 3PO was conjugated through an acid-labile hydrazone bond. The optimal micelle formulation was determined following the screening of block copolymer library modified with various aromatic and aliphatic pendant groups. Both physical drug entrapment and chemical drug conjugation methods were tested to maximize 3PO loading in the micelles during the screening. Results: Particulate characterization showed that the PEG-p (HYD) block copolymers conjugated with 3PO (2.08?2.21 wt. %) appeared the optimal polymer micelles. Block copolymer compositions greatly affected the micelle size, which was 38 nm and 259 nm when 5 kDa and 12 kDa PEG chains were used, respectively. 3PO release from the micelles was accelerated at pH 5.0, potentiating effective drug release in acidic tumor environments. The micelles retained biological activity of 3PO, inhibiting various cancer cells (Jurkat, He-La and LLC) in concentration ranges similar to free 3PO. Conclusion: A novel micelle formulation for controlled delivery of 3PO was successfully prepared. Springer Science+Business Media, LLC 2011.

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A composition for the delivery of nucleic acid to target cells or tissues, which comprises polycationically charged polymer as a carrier of nucleic acid is provided. Said polycationically charged polymer is a polymer which may comprise a charged polymer segment having a main chain based on poly(amino acid), polysaccharide, polyester, polyether, polyurethane or vinyl polymer and having, as a side chain, a group of formula -NH-(CH2)a-(NH(CH2)2)e-NH2 (wherein a and e independently denote an integer of 1 to 5) which is connected to said main chain either directly or via a linker. This composition is low-toxic, and has a high efficiency in introducing nucleic acid into cells.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2396NO – PubChem