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1.
Park JB 《Natural product research》2012,26(16):1465-1472
Moschamine is a phenylpropenoic acid amide found in plants. In this article, the synthesis and two biological activities (serotoninergic and cyclooxygenase (COX) inhibitory activities) and bioavailability of moschamine were described. Moschamine was synthesised and confirmed using NMR spectroscopic methods. Using the moschamine synthesised, serotoninergic and COX inhibitory activities were investigated. At the concentration of 10?μmol?L?1, moschamine was able to inhibit forskolin-stimulated cAMP formation by 25% (p?0.015), via inhibiting serotonin receptors in the OK cells. The inhibition was repressed by two 5-HT1 antagonists (Nan-190 and spiperone), suggesting that moschamine may suppress cAMP formation via binding to 5-HT1 receptors in the cells. Also, moschamine was a very potent compound that is able to inhibit COX-I by 58% (p?0.012) and COX-II by 54% (p?0.014), at the concentration of 0.1?μmol?L?1. The oral bioavailability of moschamine was also determined in mice. 相似文献
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Françoise M. Perron-Sierra Mike Burbridge Christophe Péan Gordon C. Tucker Patrick Casara 《Tetrahedron letters》2004,45(21):4163-4166
A preparative scale synthesis of a dioxan sialic acid analog was achieved from d-mannose. The conformation and the acidic character of this dioxan derivative, closely related to sialic acid, provides a scaffold for drug design. 相似文献
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The synthesis of the rare bioactive phenylpropanoid ester known as cimiracemate B (1) from black cohosh, Cimicifuga racemosa, is described. The procedure employs a coupling method using 1, l'-carbonyldiimidazole and methyltrifluoromethanesulfonate as coupling reagents in the presence of N-methylmorpholine. 相似文献
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The synthesis of cleonine, amino(1-hydroxycyclopropyl)acetic acid, a novel amino acid contained in cleomycin, a new bleomycin-phleomycin group antibiotic, is described. 相似文献
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Jun-hua Shi Yuxun Zhou Ming-lei He Jian Jin Yi-chuan Xiao Jun-hua Xiao Dong-zhi Wei 《Chemistry of Natural Compounds》2006,42(3):325-327
A novel compound, biotinylated 18β-glycyrrhetinic acid (BGA), was synthesized. It is a compound of 18β-glycyrrhetinic acid linked with biotin.
Published in Khimiya Prirodnykh Soedinenii, No. 3, pp. 266–267, May–June, 2006.
An erratum to this article is available at . 相似文献
7.
Marimganti S Yasmeen S Fischer D Maier ME 《Chemistry (Weinheim an der Bergstrasse, Germany)》2005,11(22):6687-6700
The synthesis of the omega-amino acid 4 is described utilizing a two-dimensional synthesis strategy combined with an enzymatic differentiation of homotopic ester groups. The amino acid 4 features two non-bonded interactions that result in conformational constraints on a cyclic construct. This amino acid was incorporated into the four macrolactams 17, 22, 31, and 37. The ring in 17 and 22 is 18-membered, whereas 31 and 37 have a 19-membered ring. The pairs with the same ring size differ in a N-methyl group. For the larger macrolactams (31 and 37) conformational analysis showed that the macrocyclic rings are somewhat more rigid than in the natural lead, the depsipeptide jasplakinolide. Nevertheless, their conformations are comparable to the natural product. There are no intramolecular hydrogen bonds, neither is the cis-rotamer populated in the N-methyl compound 37. Due to the increased flexibility of the smaller macrolactams 17 and 22 and signal overlap, a distinct solution structure could not be obtained for these compounds. The amino acid 4 should be useful for restricting the conformation of other small peptides. 相似文献
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The enantioselective synthesis of (2S,3R)-3-hydroxy-3-methylproline (3) was achieved by the Sharpless AD, regioselective opening of cyclic sulfate by NaN(3) and intramolecular ring-closing reaction. The reported route has the advantage of a high overall yield and good enantiomeric purity, as well as starting from readily available chemical substrates and inexpensive reagents. 相似文献
9.
Zaijun Lu Xiaoyu Huang Junlian Huang Guangqin Pan 《Macromolecular rapid communications》1998,19(10):527-531
A new diblock copolymer of isoprene (I) and methacrylic acid (MAA) was prepared by combination of an anionic mechanism with a charge transfer complex mechanism. In the first step, the polyisoprene (PI) macroanion formed by initiation with butyllithium was capped by p-dimethylaminobenzaldehyde (capped polyisoprene = PId); a dimeric coupling product was not detected. Then the binary system constituting of PId and benzophenone was used to initiate the polymerization of MAA under UV irradiation. The resulting diblock copolymer (PI-b-PMAA) was characterized by IR, NMR and gel permeation chromatography (GPC) in detail. 相似文献
10.
A novel reactive polycarboxylic acid dye was synthesized by the reaction of polymaleic anhydride(PMA) with 3-methyl-1-(4- sulfonylphenyl)-4-(4-aminophenylazo)-2-pyrazoline-5-one.The structure of the novel dye was characterized by FTIR,UV-vis and 13C NMR spectra.The dyeing properties of dye on cotton were tested,and the novel dye possessed high fixation and good fastness. 相似文献
11.
Sarah Roberts 《Tetrahedron letters》2010,51(13):1779-4715
Since aminoglycosides have been known to exert their antibacterial activities by binding to various RNA targets, 2-deoxystreptamine served as a particularly important model in understanding RNA-small molecule interaction. Herein, 2,4,5-triaminocyclohexanecarboxylic acid was prepared as a novel 2-deoxystreptamine (2-DOS) mimic, which replaces highly flexible glycosidic bonds of aminoglycosides with amide bonds and may improve binding selectivity toward RNA targets through increased rigidity and additional hydrogen-bonding capability. This unnatural g-amino acid can also be used as a potential component for synthetic foldamers. 相似文献
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A short and stereoselective synthesis of (3R∗,4R∗,7R∗)-3,7-epoxy-4,8-dimethyl-8-nonen-4-olide, a natural product isolated from cured tobacco leaves, has been completed in six steps and 22% overall yield. A samarium(II) iodide mediated reductive cyclisation has been used to construct the functionalised tetrahydropyranol core and subsequent sequential stereoselective addition of methyllithium and lactonisation furnished the natural product. 相似文献
13.
The novel sponge alkaloid aaptamine has been synthesized for the first time by an efficient route starting from 6-methoxy-7-hydroxy-3,4-dihydrolsoquinoline. 相似文献
14.
Kenichi Yamamoto Masayoshi Nishino Yasuyuki Kato Takeo Yoshioka Yasutaka Shimauchi Tomoyuki Ishikura 《Tetrahedron letters》1982,23(50):5339-5342
Synthesis of optically active 6-phthalimidocarbapenems from 6-aminopenicillanic acid is described. 相似文献
15.
Naohiko Yasuda 《Journal of heterocyclic chemistry》1985,22(2):413-416
A convenient general method for the synthesis of unsymmetrical imidazole-4,5-dicarboxylic acid derivatives is described. The key intermediates are 5,10-dioxo-5H,10H-diimidazo[1,5-a:1′,5′-d[pyrazine-1,6-dicarboxylic acid, -1,6-dicarboxylic ester and -1,6-dicarboxamide. 相似文献
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Brian E. Kornberg Sham S. Nikam Michael F. Rafferty 《Journal of heterocyclic chemistry》1999,36(5):1271-1277
This paper describes the synthesis of several new 2,3-dimethoxy-6-methyl-7-nitro-quinoxaline-5-carboxylic acid derivatives ( 13a-m ) via a multistep synthetic route from 5-methyl-1H-benzo[d][1,3]oxazine-2,4-dione ( 1 ). 相似文献
19.
We report a GC-MS method for the simultaneous analysis of proteins oil, and diterpenoid resins found in cultural objects. The method was initially designed for protein analysis of protenaceous paints and adhesives and involves acid hydrolysis as the first step. The amino acids in the protein hydrolysates, thus obtained, are treated with propan-l-ol/ hydrogen chloride and then pentafluoropropionic anhydride. The procedure was found also to yield the propyl esters of fatty acids derived from lipids and diterpenoid acids derived from natural resins, and thus allows the choice of a single method for the analysis of artists media which contain either oil s or proteins or mixtures of both proteins and oils or even resins. Thus natural mixtures such as egg yolk and also mixtures made by the artist such as animal glue/seed oil emulsions can be analysed. Coupled with FTIR analysis of paints and the staining of cross sections, to indicate layer structure the method can help to elucidate the paints and adhesives used by artists. 相似文献
20.
A novel trinucleating ligand system H4(PDK), for porphyrin-based diamine bis(Kemp's triacid)imide, was constructed by using two molecules of Kemp's triacid and one molecule of porphyrin as building blocks. The dimeso-substituted octaalkylporphyrin unit, carrying bromomethyl groups at the ortho positions of two trans-positioned meso-phenyl groups, was synthesized from (3,3'-diethyl-4,4'-dimethyl-2,2'-dipyrrolyl)methane and (alpha-bromo-o-tolualdehyde. The structures of both of the two atropisomers (alpha,alpha- and alpha,beta-) of bromoporphyrin, H2(alpha,alpha-BP) and H2(alpha,beta-BP), were determined by X-ray crystallography, with the alpha,beta-isomer as the free base form and the alpha,alpha-isomer as the zinc complex. Both the alpha,alpha- and alpha,beta-isomers of the bromomethyl porphyrins were converted to their aminomethyl derivatives, H2(alpha,alpha-AP) and H2(alpha,beta-AP), through the corresponding imidoporphyrin intermediates, H2(alpha,alpha-IP) and H2(alpha,beta-IP), by the Gabriel synthesis. The alpha,alpha- and alpha,beta-aminoporphyrins were coupled with Kemp's triacid anhydride-chloride to form H4(alpha,alpha-PDK) and H4(alpha,beta-PDK), respectively. Unlike the alpha,beta-isomer, the structure of which was determined by X-ray crystallography for the zinc complex, H4(alpha,alpha-PDK) has a remarkable and complicated solvent-dependent 1H NMR spectrum that suggests the existence of hydrogen bonding interactions between two convergent, tethered Kemp's triacid units, as predicted in a modeling study. The convergent feature is essential for the target ligand H4(alpha,alpha-PDK) to form trinuclear metal complexes with a bis(carboxylato) dimetallic unit sitting above a metalloporphyrin ring. 相似文献