抗炎新药Acetamide45对化合物48/80诱发的皮肤瘙痒的作用机制研究

目的探讨抗炎新药Acetamide45对化合物48/80诱发的皮肤瘙痒的作用机制。方法将ICR小鼠随机分成生理盐水组、模型组(生理盐水+化合物48/80)、美吡拉明阳性对照组及Acetamide450.1、0.3、1、3mg/kg剂量组,背部皮下注射化合物48/80或组胺诱发小鼠的瘙痒行为,观察给药前、后小鼠的瘙痒次数。结果与组胺H1受体拮抗药美吡拉明相仿,腹腔内注射Acetamide45不仅可剂量依赖性地抑制由化合物48/80诱发的小鼠瘙痒行为(P<0.05),而且对组胺诱发的瘙痒行为有效(P<0.05)。结论Acetamide45作为一种新型抗炎药,能明显改善化合物48/80诱发的瘙痒行为,其作用可能通过其抑制组胺的释放及阻滞H1受体相关。本研究为Acetamide45早日应用于临床提供了初步证据。

Transfer kinetics of phenol between aqueous phase and N,N-di(1-methyl-heptyl) acetamide in kerosene

The transfer kinetics of phenol between aqueous phase and N,N di(methyl heptyl) acetaminde (N503) in kerosene has been studied using Lewis cell technique. The effects of the factors including the concentrations of phenol in aqueous phase and organic phase, the concentration of N503 in organic phase, the acidity of aqueous phase, the stirring speed and the temperature on the rates of forward and backward extraction of phenol have been examined. The regularity of extraction rate has been obtained. According to experimental results, the rates of both forward and backward extraction of phenol might be controlled by diffusion process. The diffusion step of phenol from aqueous phase to interface for forward extraction and from interface to aqueous phase for backward extraction might be the rate controlling steps.

Synthesis,Crystal Structure and Fluorescent Property of a Lanthanum(Ⅲ) Complex Coordinated with Quinolinyloxy Acetamide Ligand

A novel lanthanum（III） complex, [LaL2（NO3）3].H2O （1） based on L （L = N-（na- phthalene-l-yl）-2-（quinolin-8-yloxy）acetamide）, was synthesized and characterized by X-ray diffraction. The crystal of I belongs to the monoclinic system, space group C2c with Mr= 1017.69, a = 25.1438（17）, b = 13.5950（9）, c = 18.2349（12） A, β= 132.4980（10）° V= 4595.8（5） A3, Z= 4, Dc = 1.471 Mg/m3, F（000） = 2056,μ= 1.004 mm-1, R = 0,0588 and wR = 0.1402. The central La（lI1） ion is coordinated to four oxygen atoms, two nitrogen atoms from two independent acetarnide ligands and six oxygen atoms from three nitrate anions, possessing a distorted icosahedron coordination geometry. In the crystal of 1, intermolecular N-H……O hydrogen bonds linked the molecules into chains along the c axis. In solid state and CH3CN solution, complex 1 exhibits stronger fluorescent emission than the ligand L.

STUDIES ON THE SYNTHESIS AND REACTIONWITH ALKOXIDES OF 3－OXO－1，2－BENZOISOTHIAZOLINE－2－ACETAMIDE1，1－DIOXIDES

New 3 -oxo-benzoisothiazoline-2-acetamide 1, 1-dioxides (IIa-b) ware synthesizedand whose reaction with alkoxides was studied. The reaction results indicated that differentproducts were obtained owing to the different time of reaction with alkoxides

VINYL RADICAL POLYMERIZATION INITIATED WITH CERIC ION AND N-(SUBSTITUTED PHENYL) ACETAMIDE SYSTEMS

The polymerization of acrylamide (AAM)in H_2O/DMF or in H_2O/CH_3CN mixed solvent initiated with ceric ion (Ce^(4+) )/N-(substituted phenyl)-acetamide systems have been studied. The redox polymerization was revealed by the low value of overall activation energy (E_α) of AAM polymerization using ceric ion/N-(substituted phenyl) acetamide system as an initiator. The end group of polymer formed was detected by IR spectrum analysis method, it revealed the presence of N-(m-acetoxy-methylphenyl) acetamide (m-AAe) moiety end group in the polymer obtained with ceric ion/m-AAe initiation system.

Rate Enhancements in the Acetylation and Benzoylation of Certain Aromatic Compounds with Vilsmeier-Haack Reagents Using Acetamide, Benzamide and Oxychlorides under Non-Conventional Conditions

Acetylation and benzoylation reactions of certain aromatic aldehydes, ketones with Vilsmeier-Haack Re- agents using Acetamide and Oxychloride (SOCl2 or POCl3) under conventional (thermal) and non conven- tional [microwave irradiated (MIR), ultrasonic assisted and solvent free mortar pestle (grinding)] conditions. Reactions afforded good to excellent yields of products with both the VH reagents, reaction times were fairly less in the case of [amide/POCl3] than those of [amide/SOCl2] reagent. Reactions are dramatically acceler- ated in under sonicated and microwave irradiations with a trend: MIR (few seconds) >> Sonication (minutes) > Grinding (min) >> thermal (several hrs).

N,O-Bis(trimethylsilyl)acetamide/N-hydroxysuccinimide ester(BSA/NHS) as coupling agents for dipeptide synthesis

A method using N,O-bis（trimethylsilyl）acetamide/N-hydroxysuccinimide ester（BSA/NHS） as coupling agents for dipeptide synthesis is descried. The coupling reaction between N-hydroxysuccinimide（NHS）esters and amines could be performed under mild conditions with N,O-bis（trimethylsilyl）acetamide（BSA） as coupling reagent and no additional acid/base is required. All byproducts and excessive reactants are water soluble or hydrolysable and easy to eliminate through water-washing at the purification stage.Moreover, all the reactants are inexpensive and widely used in conventional drug production.

Antiviral and Antibacterial Activities of N-（4-Substituted phenyl） Acetamide Derivatives Bearing 1,3,4-Oxadiazole Moiety

In this paper, a series of N-（4-substituted phenyl） acetamide derivatives bearing 1,3,4-oxadiazole moiety were synthesised. Preliminary bioassays revealed that these compounds not only exhibited favourable antiviral activities toward tobacco mosaic virus （TMV） but also demonstrated sustained inhibition activities against plant pathogenic bacteria, including Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. cit- ri. Among the derivatives, TC8 and TC20 exerted the strongest curative activities against TMV, with half-maximal effective concentration （EC50） values of 239.5 and 236.2μg/mL, respectively, which were comparable to that of ningnanmycin （EC50=273.2μg/mL）. Given their simple synthesis, the target compounds can serve as alternative antiviral candidates.

Synthesis of 2-Oxazolines from Ethyl α-Cyanocinnamate Derivatives with Acetamide and N-Bromosuccinimide

An efficient method for the one-pot synthesis of 2-oxazolines from ethyl a-cyanocinnamate derivatives with acetamide and N-bromosuccinimide（NBS） in the presence of K3PO4 was developed. The reaction was performed smoothly and cleanly to give 2-oxazolines in good to excellent yields（up to 95%） in acetone at room temperature. Thirteen examples were investigated and the results indicated that a large range of a-cyanocinnamate derivatives could be suitable for this method. Based on the outcomes of experiment, a possible consecutive nucleophilic addition- cyclization pathway was proposed.

Synthesis, potential anticonvulsant and antidepressant effects of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives

A new series of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives were synthesized and evaluated for their anticonvulsive activity in a pentylenetetrazole(PTZ)-evoked convulsion model and antidepressant activity in the forced swimming test(FST) model. Eleven synthesized compounds were found to be protective against PTZ-induced seizure and showed the anticonvulsant activity. In addition,four of the synthesized compounds(4l, 4m, 4p and 4q) showed potent antidepressant-like activity.Among these compounds, compound 4l was found to have the most potent antidepressant-like activity,and significantly reduced the duration of immobility time at 100 mg/kg dose level when compared to the vehicle control, which is similar to the reference drug fluoxetine.

Facile Synthesis of Unsymmetrical N-Aryl-2,2-di（1H-indol-3-yl） Acetamide Derivatives

A facile and highly efficient method has been developed for the synthesis of unsymmetrical N-aryl-2,2-di（1H-indol-3-yl）acetamide derivatives by regioselective Friedel-Crafts alkylation of the N-aryl-2-hydroxy-2-（1H-indol-3-yl） acetamide derivatives with various indoles catalyzed by 2 mol/L H2SO4 at room temperature in ashort reaction time, the yield was up to 94%.

Design, synthesis and immunomodulating activity of C-pseudonucleosides containing thiazolidin-4-one and phenyl connected by acetamide bond

Several novel C-pseudonucleosides containing thiazolidin-4-one and phenyl connected by acetamide bond were rationally designed and easily synthesized at room temperature by using the unprotected sugar aldehyde as the starting material. The effects of the compounds on Con A-induced T cell proliferation were evaluated at five concentrations of 5, 10, 25, 50, and 100 mmol/L Interestingly,compounds 7a and 8a（n = 2, R = H） exhibited immunostimulating activities, while compounds 5a, 6a（n = 1, R = H） and 7b, 8b（n = 2, R = CH3） showed immunosuppressive activities. Another two compounds 5 b and 6b（n = 1, R = CH3） had no immunomodulating activities. These initial biological results suggested that subtle structural changes to the phenyl and acetamide bond of C-pseudonucleosides could have a significant effect on T cell proliferation bias, although it was difficult to formulate a rigorous structureactivity relationship based on the observed activities.

聚(4-乙烯基吡啶丁烷磺酸)硫酸氢盐:一个高效的多相聚(离子液体)固体酸催化剂用于无溶剂条件下一锅法合成1-酰氨基-2-萘酚和取代喹啉(英文)

Poly(4-vinylpyridinium butane sulfonic acid) hydrogen sulfate has been used as an efficient dual acidic catalyst for the one-pot preparation of 1-amidoalkyl-2-naphthols and substituted quinolines under solvent-free conditions.The catalyst was characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, and thermo-gravimetric analysis. The results revealed several advantages to our new catalyst system,including its reusability,facile work-up procedure, eco-friendly reaction conditions,short reaction time,and high product yields.

A New Alkaloid from Sinomenium acutum

Sinomenium acutum is widely used in East and South Asia for the treatment of many diseases, especially rheumatoid arthritis （RA）. The chemical research on Sinomenium acutum led to the isolation of a new alkaloid compound （1）. On the basis of chemical evidences and spectral analysis, 1 was identified as N-（1, 7-dimethoxylphenanthren-2-yl）acetamide.

Synthesis of Agomelatine by One-pot Catalytic Hydrogenation and Acetylation with NiO

Nano-NiO and bulk NiO were prepared from Ni(AC)_2·4 H_2O by coordination precipitation using aqueous ammonia and by a solid state reaction, respectively. The nickel oxide particles were characterized by X-ray Diffraction(XRD) and scanning electron microscopy(SEM). The results indicate that nano-sized NiO has a crystal phase with a standard face-centered cubic lattice structure, with a mean particle diameter of about 10 nm. The evaluation of the activity of nickel oxide nanoparticles in the catalytic hydrogenation of 7-methoxy-1-naphthylacetonitrile was carried out. The results demonstrate the efficient synthesis of the title compound by a one-pot catalytic hydrogenation and acetylation with NiO. The NiO nanoparticles displayed superior catalytic activity in the synthesis of agomelatine in the one-pot reaction.The total yield of agomelatine is over 81.8% with a purity of 99.2%, as determined by HPLC. The structure of agomelatine was confirmed by IR, MS, and 1 H NMR analysis.

Synthesis,Structure and Properties of a Novel Nickel(Ⅱ) Chloride Complex Supported by Phosphine Ligands

The C-C1 bond of N-（2-chlorophenyl）acetamide （1） was successfully activated by tetrakis（trimethylphosphine）nickel（0）. The four-coordinate nickel（II） chloride complex trans- [（C6H4NHC（=O）Me）Ni（PMe3）2CI] （2） as a C--CI bond activation product was obtained without coordination of the amide group. Phosphonium salt CI[Me3P＋-ortho-C6H4NHC（=O）Me] （3） was isolated by reacting complex 2 as a starting material under 1 bar of CO at room temperature. The molecular and crystal structures of 2 were determined by single-crystal X-ray diffraction.

An efficient synthesis of bis(indolyl)methanes and N,N'-alkylidene bisamides by Silzic under solvent free conditions

An operationally simple and green method for the synthesis of a wide range of bis（indolyl）methanes,and N,N＇-alkylidene bisamides under mild conditions,with excellent yields using Silzic,has been developed.This improved method furnishes in good yields bis（indolyl）methanes derivatives starting from indole and aldehydes,or ketones,and N,N＇-alkylidene bisamides derivatives starting from acetamide and aldehydes.The catalytic system was reused up to three times with the same efficiency.

STUDY ON TERNARY SYSTEM La(NO_3)_3-CH_2CONH_2-H_2O

There are no reports about the solubility of the system La （NO3）3-CH3CONH2H2O in literature yet. In order to elucidate the physico-chemical behavior of the system and to provide some necessary data for producing the rare earth metals, we have, in this note, studied the solubility of this system at 0 and 30℃, measured the refractive indexes of the sat-

Fe-catalyzed regioselective Friedel–Crafts hydroxyalkylation of N-substituted glyoxylamide with indoles

An efficient regioselective Friedel-Crafts hydroxyalkylation of N-substituted glyoxylamide with various indoles catalyzed by Lewis acids was developed. The reactions proceeded smoothly at room temperature and the 2-hydroxy-2-（1H-indol-3-yl）-N-substituted acetamide resulted from the reactions catalyzed by FeSO4 were synthesized in excellent yields （up to 93%）. While the bisindole compounds were obtained when FeCl3 was used as a catalyst in excellent yields （up to 92%）. A possible mechanism was proposed.