Discovery of naphthalimide conjugates as fluorescent probes for α_1-adrenoceptors

α_1-Adrenoceptors(α_1-ARs), including at least three subtypes, α_(1A), α_(1B) and α_(1D), which play essential roles in G protein-coupled receptors(GPCRs), can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes(1a–1f) for α_1-ARs, including two parts, a pharmacophore(quinazoline and phenylpiperazine) for α_1-AR recognition and a fluorophore(naphthalimide) for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α_1-adrenoceptors.     

Recent development on peptide-based probes for multifunctional biomedical imaging

Peptide-based probes play prominent roles in biomedical research due to their promising properties such as high biocompatibility, fast excretion, favorable pharmacokinetics as well as easy and robust preparation. Considering the translation of imaging probes into clinical applications, peptide-based probes remain to be the most desirable and optimal candidates.     

Synthesis under Micromave Irradition and Crystal Structure of 4′-Acetylbenzo-15-crown-5thiosemicarbazone

The title compound is a bifunctional receptors including a thiourea group and a crown ether ring. Due to many possible potentials as a new class of reagents for membrane transports, ion-selective electrodes as well as reaction catalysts, the design and synthesis of bifunctional receptors for simultaneous binding of cations and anions is of ongoning interest in srpramolecular chemistry1-5. In bifunctional receptors, the binding sites for anions and cations are covalently linked so as to exhibit…     

Synthesis and Crystal Structure of N-Hydroxy-9-(3’,4’-methylene- dioxyphenyl)-1,8-dioxo-1,2,3,4,5,6,7,8,9, 10-decahydroacridine in Aqueous Media

1 INTRODUCTION Acridine derivatives are described to have many applications, such as biological fluorescent probes[1] as well as anti-tumor[2], anti-bacterial[3], anti-HIV[4] and anti-malarial[5] agents. Because of the importance of acridine derivatives, much work has been done for several decades. Among them the classical synthetic methods involve condensing functionalized anilines and o-halogeno- benzoic acid derivatives as well as several other steps resulting in the desired acridine[…     

ORGANIC PERMSELECTIVE PERVAPORATION CHARACTERISTICS OF POLY(SILYLPROPYNE) AND COPOLYMER DENSE MEMBRANES

An investigation into the organic permselective separation through poly [1-trimethylsilyl-1-propyne] (PTMSP) and (1-trimethylsily1)-1-(1-penta-methyl-disilyl)-1-propyne copoly-mer (TMSP-PMDSP) dense membranes was made to gain an insight into the effect ofthe chemical structure of membrane materials on pervaporation (PV) characteristics. Theresults show that the copolymer has a higher separation factor α_(org/water) but with a rela-tively lower value of flux J_t (g/m~2·h) than pure PTMSP. This phenomenon may be at-tributed to the introduction of side chain with large bulk volume in copolymer, whichbrought about a decrease of excess free volume and the improvement of diffesion selectivityto some extent. With the same molar concentration of organic liquids in feed, THF/watersolutions have the highest value of α_(org/water) as well as J_t in comparison with ethanol/water,iso-propanol/water and THF/water mixtures.     

Stereoselective Synthesis of (+)-Boronolide

(+)-Boronolide (1) and its deacetylated products have attracted much attention of synthetic chemists due to their diverse biological properties as well as their structural complexities.[1] Many of these reported synthesis involved dehydrogenation of δ-lactone by using benzeneseleninic anhydride or ring-closing olefin metathesis (RCM) to introduce the requisite α,β-unsaturated δ-lactone in boronolide. Here, we report the synthesis of boronolide with diastereoselective propargylation of α-hydroxy aldehyde as the key step and D-gluconolactone as the starting material.     

α-氨基酸与氯化铷在水溶液中焓相互作用参数

The mixing enthalpies of aqueous heavy rare alkali metal chloride RbC1 solutions with aqueous α-amino acid (Loglycine, L-alanine and α-aminobutyric acid) solutions, as well as the dilution enthalpies of RbC1 and α-amino acid solutions in pure water had been measured at 298.15K. The transfer enthalpies of RbCI from pure water to aqueous α-amino acid solutions could be obtained from these data. The enthalpic pair interaction parameters of RbC1 with α-amino acid in water have been evaluated according to the McMillan-Mayer theory and discussed in terms of the electrostatic interaction, structure interaction and Savage-wood group additivity mode.     

THE THEORETICAL STUDY OF ADSORPTION OF METAL IONS ON CHITOSAN

1. INTRODUCTION Chitin, the most abundant natural amino polysaccharide and estimated to be produced annually almost as much as cellulose, is well known to consist of 2-acetamido-2-deoxy-β-D- glucose through α, β(1→4) linkage. Chitin is the major source of surface pollution in coastalareas. Chitosan is the N-deacetylated derivative of chitin and their structures are shown in Fig. 1. Fig. 1 Structures of Chitin and Chitosan Because of the excellent properties such as biocompatibility…     

POLYMERIZATION OF γ-STEARYL-α,l-GLUTAMATE N-CARBOXYANHYDRIDE USING RARE EARTH COORDINATION CATALYSTS*

A rare earth coordination system was first investigated as a new type of catalyst for the ring-openingpolymerization of α-amino acid N-carboxyanhydrides (NCAs). The results for the polymerization of γ-stearyl-α,L-glutamate(SLG) NCA using neodymium acetylacetonate (Nd(acac)_3)- or neodymium tris(2-ethylhexylphosphonate) (Nd(P_(204))_3)-triethylaluminum-water as catalysts were compared with those using conventional catalysts. It was found that the helicalpoly(γ-stearyl-L-glutamate) with high molecular weight as well as narrow molecular weight distribution can be obtained inthe presence of Nd(acac)_3/AlEt_3-1/2H_2O. The polymer obtained was characterized by IR and NMR spectroscopy.     

DFT Investigation on Spectroscopic Characteristics and Photolysis Mechanisms of α-Phenoxylacetophenone

The photoinduced bond cleavage and quenching of the α-phenoxylacetophenone excitation states can serve as a template to investigate fundamental photochemical processes. In this work, the absorption and emission spectra as well as the photodecomposition mechanisms of α-phenoxylacetophenone were studied. The density functional theory(DFT) calculations revealed that: 1) the absorption spectra in methanol obtained by the M06-2X functional agree well with those by the B3LYP one; 2) the wavelength of the strongest peak acquired with the B3LYP method is slightly higher than the M06-2X one by 20.07 nm; 3) the βC–C bond in S_1 can be broken directly.     

First One-step Enantioselective Reduction of á-Haloacetophenones into Styrene Oxides using Sodium Borohydride in Water

The synthesis of enantiomerically enriched epoxides especially styrene oxides is an interesting challenge1, since they are often valuable building blocks for various fine chemical 2 products and pharmaceuticals such as β2-, β3-, and α1-adrenergic receptor agonists3, . In recent years, 4 there has been a flood of papers describing the synthetical methods of the chiral non-racemic epoxides5, . Here we firstly developed a green, simple and potential epoxidation system by 6 enantioselecti…     

芳基汞化合物的性质研究 VI.某些氯化芳基汞的紫外吸收光谱

The UV spectra of 24 substituted phenylmercuric chlorides as well as α-and β-naphthylmereuric chlorides were measured in ethanolic solutions. The effects of the substitution group on the C-Hg bond and UV spectral characterisics were discussed.     

Single-molecule imaging reveals the stoichiometry change of epidermal growth factor receptor during transactivation by β_2-adrenergic receptor

Stimulation of G protein-coupled receptors(GPCRs) can lead to the transactivation of the epidermal growth factor receptors(EGFR). The cross-communication between the two signaling pathways regulates several important physiological or pathological processes. However, the molecule mechanism underlying EGFR transactivation remains poorly understood. Here, we aim to study the GPCR-mediated EGFR transactivation process using the single-molecule fluorescence imaging and tracking approach.We found that although EGFR existed as monomers at the plasma membrane of resting cells, they became dimers and thus diffused slower following the activation of β2-adrenergic receptor(β2-AR) by isoproterenol(ISO). We further proved thatβ2-AR-mediated changes of EGFR in stoichiometry and dynamics were mediated by Src kinase. Thus, the observations obtained via the single-molecule imaging and tracking methods shed new insights into the molecular mechanism of EGFR transactivation at single molecule level.     

RESEARCHES ON CHEMICALLY MODIFIED ELECTRODES (Ⅹ)——SURFACE CHARACTERIZATION AND ION EFFECT OF PRUSSIAN BLUE MODIFIED ELECTRODE

The Prussian blue modified electrode prepared has been characterized by mcans of X-ray diffractionmethod as well as infrared spectra. The result definitely confirms that the electroactive blue film firmlyattached to Pt substrate by electrodeposition is really composed of PB, and that the specially preparedthin films on Pt possess the same crystal structure as that of the ordinary PB synthesized chemically. Avery detailed study of ion effect of supporting electrolyte strongly suggests that both reduction and oxi-dation processes of PB film are accompanied by the penetration of only cations, but not anions. Cationssuch as Na~+, as well as K~+, NH_4~+ and Cs~+ can penetrate the film, while Li~+, Ba~(2_+) and Ca~(2_+) cannot.The redox reactions of PB film has been expressed as follows:     

Synthesis and Crystal Structure of 2-Ethoxy-spiro[2H-1, 4,2-benzoxazaphosphorine-3（4H）, 1＇-Cycloheptane] 2-Oxide

1 INTRODUCTION α-Aminophosphonates are an important class of compounds since they are considered as structural analogues of the corresponding α-amino acids. Their utilities as enzyme inhibitors, antibiotics, pharma- cological agents and many other applications are well documented[1~5]. Moreover, cyclic α-amino- phosphonates, one important kind of α-aminopho- sphonates, have attracted chemists’ interests for a long time[6~11]. In order to search for potent and selec- tive herbicides a…     

可聚合脂质体的研究 Ⅰ．含共轭双炔基团的两杂性单体及其脂质体

wo aα,w-dipolar amphiphiles, 10, 12-docosadiyne-1, 22-dicarboxylicacid (DDCA) and 10, 12-docosadiyne-1, 22-diol(DDOL)were synthesized by coupling the corresponding 10-undecylcarboxylic acid and 10-undecynol, respectively. They could form hybrid liposomes when ultrasonically dispersed with dimyristoylphosphatidylcholine (DMPC) at equal molar ratio. Liposome formation was confirmed by electron microscopy, UV measurement as well as encapsulation of fluorescent probes. UV irradiation of the mixed liposomes induced the polymerization of DDCA and DDOL on the liposomes, which could be followed by UV-Vis measurement.     

A NEW SYNTHETIC ROUTE TO α-ARYL PROPIONIC ACID AND A QUANTITA-TIVE STUDY OF THE PHOTO-S_(RN)1 REAC-TION OF ARYL HALIDES WITH CAN-BANION FROM ALKYL NITRILE

A new synthetic route leading to α-(2-(6-methoxynaphthy1))-propionic acid has ben developed. Successive one-step preparation of the appropriate α-aryl propionitrile from the aryl halides with propionitrile by photo-SRN1 procedure followed by hydrolysis gives the desired α-aryl propionic acid in excellent total yield. The photostimulated reaction of 2-bromonaph-thalene with acetonitrile or propionitrile in KNH2-NH3 solution to form the corresponding nucleophilic substitution product occurs with quantum yields considerably in excess of unit, while the pseudo-first-order rate constants of the photo-SRN1 are 30.9 and 47.0×10-5mol·s-1, respectively. Definite evidence to support the excitation of ground CTC and electron transfer from anion to ArX within the complex comes from the observation of the same φ>200 and φ>313 as well as MO calculation.     

Pillararene-based fluorescent sensors for the tracking of organic compounds

Fluorescent chemosensors based on pillararene complexes represent a new, promising branch in sensor technology. Because of CH-π interactions, aliphatic chains are well suited for the columnar cavities of pillararenes and bulky or sheet-like(sub)structures can be arranged on the portals. Thus, pillararenes form versatile receptors and an alteration of the fluorescence behavior upon complexation ensures the function of these chemosensors as the reporter. Although this field of research exists only since a few years, remarkable chemosensors were developed for substances as diverse as medical drugs,biochemicals, herbicides and explosives.     

SYNTHETIC STUDIES ON BLOOD COMPATIBLE BIOMATERIALS Ⅲ. SYNTHESIS, CHARAC-TERIZATION AND ANTITHROMBOGENICITY OF DIMETHYLDIPHEN YLPOLYSILOXANE/POLY (OXYTETRAM ETHYLENE)-POLYUREA SEGMENTED COPOLYMERS

A novel class of segmented copolymers, dimethyldiphenylpolysiloxane/poly (oxytetramethylene)-polyurea (PSPEU), was synthesized from α, ω-bis (γ-aminopropyl) dimethyldiphenylpolysiloxane (APMPS), which was prepared by means of basic ring-opening copolymerization of octamethylcyclotetrasiloxane, hexaphenylcyclotrisiloxane and 1, 3-bis (γ-aminopropyl) tetramethyl disiloxane. The relationships between the diphenylsiloxy contents and the properties of APMPS, including refractive index, glass transition temperature, solubility parameter as well as thermal stability, were investigated; meanwhile, the thermal stability, dynamic mechanical properties, mechanical properiesas well as the antithrombogenicity in vitro of the PSPEU were also revealed.     

Synthesis of α-Bromine- Terminated Polystyrene Macroinitiator and Its Initiation of MMA Polymerization by ATRP

In the present paper the synthesis of block copolymers via the transformation from living anionic polymerization (LAP) to atom transfer radical polymerization (ATRP) was described. Α-Bromine-terminated polystyrenes(PStBr) in the LAP step was prepared by using n-BuLi as initiator, tetrahydrofuran (THF) as the activator, α-methylstyrene (α-MeSt) as the capping group and liquid bromine (Br2) as the bromating agent. The effects of reaction conditions such as the amounts of α-MeSt, THF, and Br2 as well as molecular weight of polystyrene on the bromating efficiency (BE) and coupling extent (CE) were examined. The present results show that the yield of PStBr obtained was more than 93.8% and the coupling reaction was substantially absent. PStBr was further used as the macroinitiator in the polymerization of methyl-methacrylate(MMA) in the presence of copper(Ⅰ) halogen and 2,2-bipyridine(bpy) complexes. It was found that the molecular weight of the resulted PSt-b-PMMA increased linearly with the increase of the conversion of MMA and the polydispersity was 1.2-1.6. The structures of PStBr and P(St-b-MMA) were characterized by 1H NMR spectra.