N-(1,3,4-噻二唑-2-基)-N′-芳酰基脲的合成及其生物活性

2-氨基噻二唑与芳酰基异氰酸酯反应合成了13种N-(1,3,4-噻二唑-2基)-N'-的芳酰基脲,产率为54.5%～86.2%. 用核磁共振氢谱、红外光谱和元素分析确证了目标化合物的结构,室内的生物活性测定试验表明,目标化合物中的2b、2c、2e和2h具有优良的植物生长调节活性.

Synthesis and Antibacterial Activities of Erythromycin Derivatives

Aim To synthesize 4″-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4″-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, ~ 1 H NMR and ~ 13 C NMR, and the synthetic conditi...

生长激素释放肽及非肽促泌素的研究应用进展

目的：介绍９０年代发展起来的新合成生长激素释放肽（ＧＨＲＰｓ）及非肽促泌素的研究应用进展。方法：根据１９９０～１９９７年有关文献，综述这类新药的生物活性、作用机制和药效学的研究发展及其在生命科学领域中的应用。结果：生长激素释放肽６，生长激素释放肽２，生长激素释放肽１，海沙瑞林以及非肽促泌素ＭＫ０６７７和Ｌ６９２，４２９等均具有显著的释放生长激素的作用和疗效。结论：合成的生物活性肽以生长激素释放肽６和海沙瑞林具有较广阔的应用前景。

Synthesis and activity of hydroxyethylene peptidomimetic inhibitors of humanβ-secretase

A series of β-secretase peptidomimetic inhibitors with Leu＊Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% （10 mg/mL）. Compound N9 might be further modified by means of computational chemical methodology.

Efficient Syntheses of Permethylated Derivatives of Neolamellarin A,a Pyrrolic Marine Natural Product

The pyrrole-derived alkaloids with marine origin, especially their permethyl derivatives, have unique structures and promising biological activities. Marine natural product neolamellarins are a collection of lamellarin-like phenolic pyrrole compounds, which can inhibit hypoxia-induced HIF-1 activation. Many pyrrole-derived lamellarin-like alkaloids show potent MDR reversing activity. In this study, five permethylated derivatives of neolamellarin A were synthesized with their MDR reversing activity studied in order to identify new MDR reversal agents. A convergent strategy was adopted to synthesize the permethylated derivatives of neolamellarin A. Pyrrole was first converted into a corresponding N-trisisopropylsilyl （TIPS）-substituted derivative, then through iodination afforded 3,4-diiodinated pyrrole compound. The key intermediate, 3,4-disubstituent-lH-pyrrole, was obtained through desilylation of 3,4-disubstituent-l-TIPS pyrrole, which was prepared from 3,4-diiodinated pyrrole derivative and aryl boronic acid ester through Suzuki cross-coupling reaction between them. Then, the intermediate, 3,4-disubstituent-lH-pyrrole, reacted with fresh phenylacetyl chloride under n-BuLi/THF condition afforded the target compounds. Finally, we obtained five novel pyrrolic com- pounds, permethylated derivatives ofneolamellarin A 16a-e, in 30%-37% yield through five step reactions. The bioactivity testing of these compounds are in process.

Polypeptide from Chlamys farreri inhibits UVB-induced apoptosis of HaCaT cells via iNOS/NO and HSP90

Polypeptide from Chlamys farreri(PCF) is a novel marine bioactive product that was isolated from the gonochoric Chinese scallop Chlamys farreri,and was found to be an effective antioxidant in our recent studies.In this study,we investigated the effect of PCF on ultraviolet B(UVB)-induced apoptosis of HaCaT cells and the intracellular signaling pathways involved.Pretreatment with the inducible nitric oxide synthase(iNOS) inhibitor S-methylisothiourea sulfate inhibited UVB-induced apoptosis,indicating that iNOS and NO play important roles in apoptosis.On the other hand,the inhibition of UVB-induced apoptosis in the immortalized keratinocyte(HaCaT) cells by PCF was estimated using a DNA ladder.PCF treatment inhibited UVB-induced iNOS activation,as determined by RT-PCR,NO production,as determined by ESR,and up-regulated heat shock protein(HSP) 90 activation,as determined by Western blotting.Our results indicate that iNOS and NO are involved in UVB-induced apoptosis of HaCaT cells and the protective effect of PCF against UVB irradiation is exerted by suppressing the expression of iNOS,followed by inhibition of NO release and enhanced activation of HSP90.

Effect of Salinity on the Biosynthesis of Amines in Litopenaeus vannamei and the Expression of Gill Related Ion Transporter Genes

This study examined the effect of salinity on the expression of Na+/K+-ATPase(NKA) α-subunit and vacuolar-type H+-ATPase(V-ATPase) β-subunit gene in the gill of Litopenaeus vannamei. Semi-quantitative reverse transcription-polymerase chain reaction(RT-PCR) assay showed that the expression of NKA α-subunit and V-ATPase β-subunit gene was significantly influenced by salinity. It was found that the NKA activity significantly varied with salinity in time and dose dependent manner; whereas the V-ATPase activity did not. The abundance of NKA α-subunit gene transcript increased rapidly when the salinity decreased from 26 b to 21, and slowly when the salinity decreased from 26 to 31 within the first 24 h. When the salinity decreased from 26 to 21, the transcription of NKA α-subunit gene in gill epithelium was higher at 12 h than that at 0 h, which was consistent with the result of immunoblotting assay of NKA α-subunit. In addition, salinity had a significant time- and dose-dependent effect on the concentration of biogenic amines in both hemolymph and gill. As compared to other parameters, the concentration of dopamine(DA) and 5-hydroxytryptamine(5-HT) varied in different patterns when the salinity decreased from 26 to 21 or increased from 26 to 31, suggesting that DA and 5-HT played different regulatory roles in osmotic adaption and modulation of shrimp when salinity varies.

Design and Synthesis of Novel Fluorine-containing Acrylates

A series of novel fluorine-containing acrylates 6a-6g were synthesized via the condensation of ethyl cyanoacetate and trifluoroacetic anhydride, followed by chloridization and the coupling reaction with amines. These new compounds exhibited some biological activity as preliminary bioassay indicated. A plausible reaction mechanism was outlined and discussed.

The Dependence of the Dissociation Rate of Methane-SDS Hydrate below Ice Point on Its Manners of Forming and Processing

The dissociation rates of methane hydrates formed with and without the presence of sodium dodecyl sulfate （methane-SDS hydrates）, were measured under atmospheric pressure and temperatures below ice point to investigate the influence of the hydrate production conditions and manners upon its dissociation kinetic behavior. The experimental results demonstrated that the dissociation rate of methane hydrate below ice point is strongly dependent on the manners of hydrate formation and processing. The dissociation rate of hydrate formed quiescently was lower than that of hydrate formed with stirring; the dissociation rate of hydrate formed at lower pressure was higher than that of hydrate formed at higher oressure; the comoaction of hydrate after its formation lowered its stability, i.e., increased＇its dissociation rate.The stability of hydrate could beincreased by prolonging the time period for which hydrate was held at formation temperature and pressure before it was cooled down, or by prolonging the time period for which hydrate was held at dissociation temperature and formation pressure before it was depressurized to atmospheric pressure. It was found that the dissociation rate of methane hydrate varied with the temperature （ranging from 245.2 to 272.2 K） anomalously as reported on the dissociation of methane hydrate without the presence of surfactant as kinetic promoter. The dissociation rate at 268 K was found to be the lowest when the manners and conditions at which hydrates were formed and processed were fixed.

Synthesis and Properties of 1,3-bis-adamantyl Disubstituted Ureas and Biureas

1,3-disubstituted ureas of adamantine series are potent for hypertension and inflammatory treatment. The most valuable parameters of these compounds are melting point and solubility. Higher melting point leads to lower bioavailability and for most of the compounds investigated before it was very high. Usage of isocyanates containing 1,3-dimethyladamantane fragment will significantly decrease the melting point, improve solubility and therefore improve bioavailability of 1,3-disubstituted ureas and other biologically active compounds produced on its base. This article presents new 1,3-disubstituted ureas and biureas synthesized by the authors.

Syntheses and Crystal Structures of Bis-[oxo-bis(p-ferrocenylbenzoxy di-n-propyltin)](I) and Bis[oxo-bis(β-ferrocenoylpropionyloxy di-n-propyltin )](II)

Bis-[oxo-bis(p-ferrocenylbenzoxy di-n-propyltin)] I and bis-[oxo-bis(-ferrocenoyl- propionyloxy di-n-propyltin)] II were synthesized and their crystal structures have been determined by X-ray diffraction analysis. The compound I2C6H6 ([(FcC6H4COOSnPr2)2O]22C6H6 or C92H108Fe4O10Sn42C6H6, Mr = 2384.16) is of triclinic, space group P?with a = 12.826(4), b = 13.099(5), c = 17.539(5) ? = 78.229(5), ?= 71.852(5), = 62.746(5)? V = 2483(1) ?, Z = 1, Dc = 1.490 g/cm3, = 0.71073 ? (MoK? =1.611 mm-1 and F(000) = 1128. The structure was refined to R = 0.0491 and wR = 0.1053 for 4690 unique reflections with I > 2(I). The compound IIC6H6 ([(FcCOCH2CH2COOSnPr2)2O]2C6H6 or C80H108Fe4O14Sn4C6H6, Mr = 2115.93) is of triclinic, space group P?with a = 11.260(4), b = 14.126(5), c = 15.961(6) ? = 91.400(6), = 110.654(6), = 104.931(6), V = 2277(1) 3, Z = 1, Dc = 1.510 g/cm3, = 0.71073 ? (MoK? = 1.750 mm-1 and F(000) = 1046. The structure was refined to R = 0.0466 and wR = 0.1138 for 5061 unique reflections with I > 2(I). The two compounds have the similar structures: both are dimers containing centrosymmetric Sn2O2 cores. But there are some differences in the ligating modes between the carboxylate groups and the Sn atoms.

3D Photo-Fabrication for Tissue Engineering and Drug Delivery

The most promising strategies in tissue engineering involve the integration of a triad of biomaterials, living cells, and biologically active molecules to engineer synthetic environments that closely mimic the healing milieu present in human tissues, and that stimulate tissue repair and regeneration. To be clinically effective, these environments must replicate, as closely as possible, the main characteristics of the native extracellular matrix(ECM) on a cellular and subcellular scale. Photo-fabrication techniques have already been used to generate 3D environments with precise architectures and heterogeneous composition, through a multi-layer procedure involving the selective photocrosslinking reaction of a light-sensitive prepolymer. Cells and therapeutic molecules can be included in the initial hydrogel precursor solution, and processed into 3D constructs. Recently, photofabrication has also been explored to dynamically modulate hydrogel features in real time, providing enhanced control of cell fate and delivery of bioactive compounds. This paper focuses on the use of 3D photo-fabrication techniques to produce advanced constructs for tissue regeneration and drug delivery applications. State-of-the-art photo-fabrication techniques are described, with emphasis on the operating principles and biofabrication strategies to create spatially controlled patterns of cells and bioactive factors. Considering its fast processing, spatiotemporal control, high resolution, and accuracy, photo-fabrication is assuming a critical role in the design of sophisticated 3D constructs. This technology is capable of providing appropriate environments for tissue regeneration, and regulating the spatiotemporal delivery of therapeutics.

Synthesis and Crystal Structure of 3,3′-(Hexane-1,6-diyl)bis(1-acetyl-5,5-dimethylhydantoin),a New Inducer of Differentiation

The title compound (C20H30N4O6, Mr = 422.48) was synthesized and its crystal structure was determined by X-ray diffraction method. It crystallizes in the triclinic system, space group P with cell parameters: a = 8.330(2), b = 8.468(2), c = 16.017(3) ? ?= 97.30(3), ?= 92.33(3), ?= 103.94(3)? V = 1084.7(4) ?, Dc = 1.294 g/cm3, Z = 2, F(000) = 452 and ?= 0.096 mm-1. The structure was refined to R = 0.0483 for 3732 observed reflections with I > 2s(I) and wR = 0.1335 for 4828 unique reflections. The hydantoin rings are planar and the two ring planes of one molecule are paralleled to each other.

Chemical Interaction UO2Cl2 with α-and β-Amino Acids in Aqueous and Organic Solution

This paper presents the results of the search of biologically active uranium compounds such as amino acids. We first received and examined X-ray and IR （infrared radiation） spectroscopy of uranium complexes with α- and β-amino acids in aqueous and organic solution. We proposed a method for direct synthesis of complex organic compounds of uranium chloride UO2Cl2 with α- andβ-amino acids for the synthesis of drugs for the treatment of cancer.

Physicochemical Parameters for Biological and Synthetic Surfactants Used as Detergents

Biological and synthetic surfactants were compared in terms of their ability to reduce interfacial tension, change the thermodynamic characteristics of a pre-conditioned surface, and to modify the rheological properties of their respective formulations at two different temperatures. Both classes of suffactants were able to reduce the inteffacial tension of their formulations to a similar level. However, the biosurfactants were more effective than the synthetics surfactants. Biosurfactants also altered the surface properties of stainless steel, rendering it hydrophilic. Microbial adhesion to stainless steel conditioned with biosurfactants was found to be thermodynamically unfavorable for all microbial strains tested. A linear relationship between shear stress and shear rate was obtained across a range of experimental conditions for all surfactant mixtures, indicating that all formulations behaved as Newtonian fluids.

Synthesis and Biological Activity Study of New Schiff and Mannich Base Ligands Derived from Isatin and 3-Amino-1,2,4-triazole and Their Metal Complexes

Two new Mannich and Schiff base ligands namely： （1-（3＇-amino-methyl-1＇（H）-1＇,2＇,4＇-triazole）-3-（1＇（H）-l＇,2＇,4＇- triazole-3＇-yl） iminoisatin （Lt） and l-morpholinomethyl-3-（1＇（H）-1＇,2＇,4＇-triazolyl）iminoisatin （LII） were prepared from condensation reaction of the new Schiff base 3-（l＇（H）-l＇,2＇,4＇-triazole-3＇-yl）iminoisatin （SBH） （0.01 mol） with formaldehyde and 3-amino-l,2,4-triazole （3-At） or with formaldehyde and morpholine （0.01 mole each） respectively. Structures were characterized by tH NMR, CHN analyses, mass spectra and IR spectra. Metal complexes were synthesized by heating each ligand （0.02 mo with metal salts （0.01 moo in ethanol or ethanol： acetone mixture respectively. The formula of metal complexes were suggested depending on CHN and thermal analyses, metal and chloride contents, IR and UV-visible spectra, magnetic moments （laefr） and conductivity measurements. All complexes were of octahedral geometry except palladium （II） complexes which were square planar. The two ligands and some selected metal complexes showed various antibacterial and cytotoxic effects.