870-46-2Relevant articles and documents
A novel poly(l -glutamic acid) dendrimer based drug delivery system with both pH-sensitive and targeting functions
Yuan, Hui,Luo, Kui,Lai, Yusi,Pu, Yuji,He, Bin,Wang, Gang,Wu, Yao,Gu, Zhongwei
, p. 953 - 962 (2010)
The functionalization of pH-sensitiveness and cellular targeting is a promising strategy to fabricate drug delivery systems with high efficiency, high selectivity and low toxicity. In this paper, a poly(l-glutamic acid) dendrimer based drug delivery system with both pH-sensitive and targeting functions is reported. Poly(l-glutamic acid) dendrimers with a polyhedral oligomeric silsesquioxane (POSS) nanocubic core were synthesized. Its globular morphology and compact structure with multiple peripheral functional groups made it suitable for drug delivery. The OAS-G3-Glu dendrimer was conjugated with doxorubicin via pH-sensitive hydrazine bonds and targeting moiety (biotin). The cellular internalization and antitumor effects of the conjugates was evaluated in vitro. Both DLS and TEM results indicated that the conjugates aggregated into nanoparticles with diameters around 50 nm. The release rates of doxorubicin at pH 5.0 were much faster than those at pH 7.0 due to the acid cleavage of the hydrazine bonds. The internalization study revealed that the cellular uptake of the biotin modified conjugates was mainly through receptor-mediated endocytosis. These results indicate that our poly(l-glutamic acid) dendrimers with OAS core are promising vectors for fabricating smart and targeting drug delivery systems.
Preparation method of high-purity tert-butyl carbazole
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Paragraph 0029-0036, (2021/09/21)
The invention relates to the technical field of drug synthesis, in particular to a preparation method of high-purity tert-butyl carbazole. After the completion of the reaction, the hydrazine monohydrate is neutralized with a base, extracted with a solvent, concentrated, and then crystallized by a weak polar solvent to give a tert-butyl carbazole product. The preparation method of the tert-butyl carbazole can obtain the high-purity product (≥ 99.5%), has high yield (≥ 90%), is simple to operate, and is suitable for industrial large-scale production.
Sitagliptin impurity and preparation method and detection method thereof
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Paragraph 0046; 0047, (2021/10/05)
The novel impurity can provide standard reference for quality control of sitagliptin and safety detection of clinical medication, so that safety and reliability of clinical medication are guaranteed. In addition, the preparation method of the impurity compound provided by the invention is simple to operate and mild in reaction conditions, can obtain impurity compounds with high purity and high yield, is used for further researching impurity properties, and provides technical support for the content control of sitagliptin compounds and the safety problems of sitagliptin. The sitagliptin impurity detection method can perform targeted qualitative detection on the impurities, is high in detection precision, and is beneficial to the technical means for detecting impurities in the sitagliptin, so that the quality of the sitagliptin impurity is controlled.
Elastic targeting polypeptide-based medicine-carrying nanoparticle as well as preparation method and application thereof
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Paragraph 0029-0031; 0039-0041, (2020/07/15)
The invention discloses an elastic targeting polypeptide-based medicine-carrying nanoparticle. The nanoparticle is prepared from an elastic targeting polypeptide and a modified medicine, wherein the modified medicine is a modified paclitaxel PTX-LEV-MECH or modified salinomycin Sail-ABA-MPBH. The elastic targeting polypeptide-based medicine-carrying nanoparticle provided by the invention is 100nmor below in particle size, so that the dispersion degree is low, the medicine carrying rate is high, and the nanoparticle can be combined with in-vivo albumin for transferring and carrying medicine, and also can be combined with acidic rich cysteine specifically secreted by tumor cells, the drug is concentrated in the acidic environment, the breast cancer in-situ cancer is targeted for killing, and the toxic and side effects of the drug on the whole body are reduced; and the efficacy of treating breast cancer is increased and improved by utilizing the synergistic effect of two nanoparticles, the occurrence of the metastasis of the breast cancer cells through a lymphatic system and a blood system is reduced, and the occurrence of serious complications such as medical-source lymphatic edemacaused by a lymph node sweeping surgery is reduced.
Synthesis method of single BOC protection double-amino compound
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Paragraph 0022; 0023, (2018/06/21)
The invention relates to the field of fine chemical engineering, in particular to a synthesis method of a single BOC protection double-amino compound. The synthesis method comprises the steps that firstly, an acid compound and double-amino are subjected to complex reaction, then moderate BOX acid anhydride is added for reaction, and a product is obtained. The method is simple in reaction step, high in product yield and purity and suitable for industrial production.
Multiprotein Dynamic Combinatorial Chemistry: A Strategy for the Simultaneous Discovery of Subfamily-Selective Inhibitors for Nucleic Acid Demethylases FTO and ALKBH3
Das, Mohua,Yang, Tianming,Dong, Jinghua,Prasetya, Fransisca,Xie, Yiming,Wong, Kendra H. Q.,Cheong, Adeline,Woon, Esther C. Y.
supporting information, p. 2854 - 2867 (2018/09/25)
Dynamic combinatorial chemistry (DCC) is a powerful supramolecular approach for discovering ligands for biomolecules. To date, most, if not all, biologically templated DCC systems employ only a single biomolecule to direct the self-assembly process. To expand the scope of DCC, herein, a novel multiprotein DCC strategy has been developed that combines the discriminatory power of a zwitterionic “thermal tag” with the sensitivity of differential scanning fluorimetry. This strategy is highly sensitive and could differentiate the binding of ligands to structurally similar subfamily members. Through this strategy, it was possible to simultaneously identify subfamily-selective probes against two clinically important epigenetic enzymes: FTO (7; IC50=2.6 μm) and ALKBH3 (8; IC50=3.7 μm). To date, this is the first report of a subfamily-selective ALKBH3 inhibitor. The developed strategy could, in principle, be adapted to a broad range of proteins; thus it is of broad scientific interest.
Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists
Schiano Moriello, Aniello,López Chinarro, Silvia,Novo Fernández, Olalla,Eras, Jordi,Amodeo, Pietro,Canela-Garayoa, Ramon,Vitale, Rosa Maria,Di Marzo, Vincenzo,De Petrocellis, Luciano
, p. 8255 - 8281 (2018/09/25)
The transient receptor potential vanilloid type-2 (TRPV2) protein is a nonselective Ca2+ permeable channel member of the TRPV subfamily, still considered an orphan TRP channel due to the scarcity of available selective and potent pharmacological tools and endogenous modulators. Here we describe the discovery of novel synthetic long-chain capsaicin derivatives as potent TRPV2 antagonists in comparison to the totally inactive capsaicin, the role of their hydrophobic chain, and how the structure-activity relationships of such derivatives led, through a ligand-based approach, to the identification of endogenous long-chain fatty acid ethanolamides or primary amides acting as TRPV2 antagonists. Both synthetic and endogenous antagonists exhibited differential inhibition against known TRPV2 agonists characterized by distinct kinetic profiles. These findings represent the first example of both synthetic and naturally occurring TRPV2 modulators with efficacy in the submicromolar/low-micromolar range, which will be useful for clarifying the physiopathological roles of this receptor, its regulation, and its targeting in pathological conditions.
Visible-light induced copper(i)-catalysed denitrogenative oxidative coupling of hydrazinylpyridines with terminal alkynes
Charpe, Vaibhav Pramod,Hande, Aniket A.,Sagadevan, Arunachalam,Hwang, Kuo Chu
supporting information, p. 4859 - 4864 (2018/11/21)
Visible light mediated copper catalysed denitrogenative oxidative coupling of 2-hydrazinopyridines with terminal alkynes to form 2-(alkyl/arylethynyl) pyridines in the presence of O2 at room temperature is reported with 42 examples. This is the first report on visible light stimulated N2 elimination by an in situ generated copper(ii) superoxo/peroxo complex. N2 and water are the only by-products. The green chemistry metrics evaluation signifies that the current method is ecofriendly and economically feasible. This method allows the green synthesis of mGluR5 receptor antagonists, 2-methyl-6-(phenylethynyl)pyridine (MPEP) and 2-((3-methoxyphenyl)ethynyl)-6-methylpyridine (M-MPEP).
The enantioselective addition of 1-fluoro-1-nitro(phenylsulfonyl)methane to isatin-derived ketimines
Urban,Franc,Hofmanová,Císa?ová,Vesely
supporting information, p. 9071 - 9076 (2017/11/14)
An asymmetric organocatalytic addition of fluorinated phenylsulfonylnitromethane to isatin-derived ketimines was developed. The reaction was efficiently catalyzed by a chiral tertiary amine, cinchonine. This methodology provides a new type of optically active compound with two adjacent quaternary carbon stereocenters in good yield (up to 96%), with moderate diastereoselectivity (up to 5.7:1 dr) and excellent enantioselectivity (up to 98/96% ee).
A reusable and naked-eye molecular probe with aggregation-induced emission (AIE) characteristics for hydrazine detection
Cheng, Xiamin,Zhang, Ruoyu,Cai, Xiaolei,Liu, Bin
, p. 3565 - 3571 (2017/07/13)
We report a fluorogenic probe for naked-eye sensing of hydrazine in solution and in the gaseous phase. The probe based on tetraphenylethylene (TPE) with aggregation-induced emission (AIE) characteristics shows OFF-ON fluorescence as observed by thin-layer chromatography (TLC) upon treatment with hydrazine. Specifically, the fluorescence of the probe was quenched due to the attached NN group, which can be reduced to -NH-NH- in the presence of hydrazine to turn on the fluorescence. The reduced intermediate can be easily oxidized in air to regenerate the original probe for recyclable usage. Both fluorometric and colorimetric readings were achieved by TLC with high sensitivity and excellent selectivity. This study thus represents a simple example of a reusable and naked-eye molecular probe for monitoring environmental hazards. Finally, the probe has also been applied to detect hydrazine in live cells.
