含酰基氨基甲酸酯基硫脲核苷类化合物的合成及生物活性

在前期核苷类化合物的研究基础之上,为了进一步改善该类化合物的生物活性,基于几丁质合成酶催化作用机制,通过活性亚结构拼接方法,将具有良好生物活性的氨基甲酸酯基片段引入到前期所设计化合物的硫脲桥当中,设计合成了一系列结构新颖的含酰基氨基甲酸酯基硫脲的核苷类化合物.以尿苷为原料,经4步反应制得目标物,其结构经IR,1H NMR及HRMS确证.初步生测结果表明,部分化合物具有一定的杀菌和杀虫活性,化合物5j对棉铃虫的抑制活性与对照药剂除虫脲相当.     

Synthesis,Structure and Properties of C(X)NHP(Y) Fragment Containing Compounds

Abstract

N-(thio)carbonyl(thio)amidophosphate, their open-chain and crown-containing analogues with a C (X) NHP (Y) fragments are associated with intermolecular hydrogen bonds as C=X…H-N and P=Y…H-N or intramolecular hydrogen bonds of N-H…O(macrocycle). These compounds easily enter into alkylation reaction, are added according to C=N bonds of activated imines, take part in O → S and S → O exchanging reactions.     

Synthesis of New Cyclopentenofullerenes Containing a Norbornene Fragment

Russian Journal of Organic Chemistry - Endic acid imides were synthesized by direct fusion of endic anhydride with various amino acids. Further transformations of the resulting acids gave new...     

Synthesis of Ketones Containing a Diphenyl Ether Fragment

Russian Journal of Organic Chemistry -     

Amphiphilic Fluorescence Resonance Energy-Transfer Dyes: Synthesis,Fluorescence, and Aggregation Behavior in Water

Amphiphilic pyrene/perylene bis-chromophore dyes were synthesized from unsymmetrically substituted perylene bisimide dyes, which were obtained through three synthetic methods. The optical and aggregation behaviors of these functional dyes were studied by means of UV/Vis absorption and fluorescence spectroscopy, dynamic light scattering, and TEM. These dyes are highly fluorescent and cover the whole visible-light region. A donor/acceptor dye displays intramolecular fluorescence resonance energy transfer (FRET), with a high efficiency of up to 96.4 % from pyrene to perylene bisimide chromophores, which leads to a high fluorescence color sensitivity to environmental polarity. Under a λ=365 nm UV lamp, the light-emitting colors of the donor/acceptor dye change from green to yellow with increasing solvent polarity, which demonstrates application potential as a new class of FERT probes. The donor/acceptor dye in water was assembled into hollow vesicles with a narrow size distribution. The bilayer structure of the vesicular wall was directly observed by means of TEM. These vesicular aggregates in water are fluorescent at λ=650–850 nm within the near-infrared region.     

Synthesis of 1,4-Naphthoquinone Derivatives Containing a Melamine Fragment

Russian Journal of Organic Chemistry -     

Synthetic Approach to the Synthesis of Physiologically Active Compounds: II. Synthesis of Disubstituted Adamantanes Containing an N-Benzoylphenylisoserine Fragment

A preparation is reported of some previously unknown 1,4-disubstituted adamantane derivatives containing a phenylisoserine fragment.     

新型苄基氨基甲酸酯类化合物的合成及其抗菌活性

以邻氯苄胺为原料,经6步反应制得中间体2-氯-5-［1-(氧丙炔基亚氨基)乙基］苄基氨基甲酸甲酯（7）;取代芳基肟经氯化后再分别与7经环合反应合成了一系列新型的苄基氨基甲酸酯类化合物（10a~10l）,其结构经¹H NMR表征。初步的抗菌活性测试表明：在用药量为200 mg·L^-1时,大部分化合物对水稻纹枯病显示出较好的抗菌活性,其中10f的抑菌活性最高,抑制率95%。     

几种具有电子给-受体结构的两亲性化合物的合成及鉴定

设计并合成了3种含有巴比妥酸基团的具有电子给-受体结构的两亲性有机分子,经元素分析、红外光谱、核磁共振谱确定了其结构,研究了醛与巴妥酸缩合的条件及醛的反应活性与其IR、NMR谱的关系.     

Molecular Daisy Chains: Synthesis and Aggregation Studies of an Amphiphilic Molecular Rod

A water‐soluble cyclophane as the loop subunit, monofunctionalized with a molecular rod, has been synthesized to introduce a new binding motif for mechanically interlinked oligomers. It has been demonstrated that this hermaphroditic compound forms [c2]daisy chains in polar solvent over a wide range of concentrations. Furthermore, evidence for the formation of higher mechanically interlinked oligomers above the critical aggregation concentration has been obtained.     

新型两亲性壳聚糖衍生物的合成、表征及对难溶性药物的增溶性

以天然可生物降解的壳聚糖为原料, 通过在壳聚糖6位羟基上引入羧甲基, 在2位氨基上引入疏水烷基链, 制得N-辛基-O,N-羧甲基壳聚糖(OCC)两亲性衍生物, 分别用FTIR、1H NMR和元素分析等技术对其结构进行表征, 用广角X射线衍射(WAXD)和差示扫描量热法(DSC)对其物理性质进行分析, 并考察其在各种溶剂中的溶解性能及其对难溶性药物的增溶能力. 所制备的OCC羧甲基取代度为115.9%, 取代主要发生在6位羟基上; 辛基取代度58.0%, 取代主要发生在2位氨基上; 与壳聚糖相比, OCC分子间/内氢键作用减弱; OCC在常用的有机溶剂中不溶, 但在水中溶解度增加, 能够形成具有淡蓝色乳光的纳米胶体溶液, 对难溶性抗肿瘤药物紫杉醇具有优越的增溶能力, 使紫杉醇在水中的溶解度提高近500倍, 载药量为34.6%(质量分数), 包封率为89.9%. OCC是潜在的优良的难溶性药物增溶载体材料.     

Synthesis,Self-Association,and Solubilizing Ability of an Amphiphilic Derivative of Poly(ethylene glycol) Methyl Ether

A new amphiphilic derivative–methoxy(polyethoxy)ethyl stearate has been synthesized with the goal of creating therefrom systems for delivery and enhancement of bioavailability of piperine. The aggregation and solubilizing properties of ω-methylpoly(oxyethylene) stearate have been studied by means of a set of physicochemical methods.     

Synthesis of New Conjugated Diynes Containing Carbamate Groups, and Study of Their Properties

Carbamates of monoacetylene and diacetylene series were synthesized and characterized. A catalytic system CuI-pyrrolidine was applied for the first time to a synthesis of symmetrical diacetylenes by oxidative dimerization of terminal acetylenes. The comparative activity of diynes obtained was studied in the photoinitiated solid-phase topochemical polymerization. Diyne carbamates undergoing thermal polymerization were obtained for the first time.     

Synthesis and Optical Properties of New Chalcones Containing a 3,4-Ethylenedioxythiophene Fragment

Russian Journal of Organic Chemistry - A new series of chalcones bearing two or more 3,4-ethylenedioxythiophene fragments were synthesized, and their optical properties were studied. The Stokes...     

Synthesis and Antimicrobial Properties of Chiral Mannich Bases Containing a Norbornene Fragment

Russian Journal of Organic Chemistry - New Mannich bases were synthesized from chiral norbornenylmethanol, secondary amines, and formaldehyde. Their structure was confirmed by elemental analyses...     

Mannich Reaction as a Convenient Route to New Macrocyclic Compounds Containing an Uracil Fragment

Mannich reaction of 1,3-bis[4-(2-mercaptomethylphenoxy)butyl]-6-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione, formaldehyde, and N-benzylamine afforded a 24-membered macrocyclic compound containing an uracil fragment, 1,3-(11-benzyl-6,7:15,16-dibenzo-5,17-dioxa-9,13-dithia-11-aza-6,15-heneicosadiene-1,21-diyl)-6-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione.     

两亲三元壳寡糖衍生物的合成及其包合物的研究

本文报道了新型水溶性甲氧基聚乙二醇-b-聚己内酯两亲嵌段共聚物接枝壳寡糖(COS-g-PCL-b-MPEG)共聚物的合成, 研究了两亲三元COS衍生物的合成及在水溶液中α-CD与其的包合作用.     

含硅有机锗化合物的合成

报道了一类含硅有机锗化合物的合成。从Ｍｅ３ＳｉＣｌ，ＲＸ，ＧｅＯ２出发，经过氯化、格氏反应、亲核取代等反应，制得目标化合物－－二〔烃基二甲硅基甲基〕锗的二氯化物。它们的结构经元素分析和红外表征。     

对甲苯烷酰胺基三苯基季膦盐的合成

以对甲苯胺为原料,氯烷酰氯为连接基团合成了4个含酰胺键的季膦盐,其结构经1H NMR,13C NMR,31P NMR,IR和MS表征。