共查询到20条相似文献,搜索用时 15 毫秒
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Rudolf Wunderlin Shub Dev Sharma Panagiota Minakakis Robert Schwyzer 《Helvetica chimica acta》1985,68(1):12-22
Asymmetric disulfide conjugates of mercaptosuccinyl tobacco mosaic virus (TMV ~ SH) with Nα-desacetyl-Nα-5-(mercaptovaleryl)-α-melanotropin were prepared via the S-sulfoderivative of the peptide. The conjugates, TMV ~ S? S ~ α-MSH(n), contained up to n = 330 disulfide-linked peptide molecules/virion. Similarly, fluorescent conjugates, Rh(m) ~ TMV ~ S? S ~ α-MSH(n) were prepared, containing m ≈? 200 rhodamine molecules linked to the virions by thiourea bridges. Such conjugates were designed to study α-MSH receptor localization and dynamics (mainly internalization), because the carrier virions which served to enhance specific receptor binding and as fluorescent or radioactive markers may be detached from the neuropeptides at will by reduction. Reduction occurred in solution and on the cell surface, but not in the cytoplasm, thus allowing detection of internalized agonist-receptor complexes. The conjugates were superpotent agonists for tyrosinase stimulation in Cloudman S-91 melanoma cell cultures, but were inactive for cyclic AMP accumulation. Their rather rapid internalization and the influence of reducing agents and other agonists on their biologic activity suggest a close connection between receptor location and biologic response as well as the presence of essential receptor HS-groups. 相似文献
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α-Methylene-γ-butyrolactones [dihydro-3-methylene-2(3H)furanones] constitute an important group of natural products and possess wide-ranging biological activities. Progress in the synthesis of the heterocycle and the classification of the synthetic methods are not only of practical interest, but also fundamentally important as a current example for the construction of an unusual 1,4-functionality distance and an α-substituted acrylic ester moiety which is susceptible to nucleophilic attack. 相似文献
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Tsutomu Oishi Minoru Fujimoto 《Journal of polymer science. Part A, Polymer chemistry》1992,30(9):1821-1830
A novel type of optically active N-[4-N′-(α-methylbenzyl)aminocarbonylphenyl]maleimide [(R)-MBCP] was synthesized from maleic anhydride, p-aminobenzoic acid, and (R)-methylbenzylamine. Radical homopolymerization of (R)-MBCP was performed in tetrahydrofuran (THF) at 50 and 70°C for 24 h to give optically active polymers having [α]25D = -141° and -129°, respectively. Anionic polymerization of (R)-MBCP with n-butyllithium in THF and N,N-dimethylformamide gave an optically active polymer having ?78 to ?81° of [α]25D. Radical copolymerizations of (R)-MBCP (M1) were performed with styrene (ST, M2) and methyl methacrylate (MMA, M2) in THF at 50°C. The monomer reactivity ratios (r1, r2) and the Alfrey-Price Q-e values were determined as follows: r1 = 0.009, r2 = 0.091, Q1 = 1.30, e1 = 1.87 in the (R)-MBCP-ST; r1 = 0.27, r2 = 1.21, Q1 = 0.93, e1 = 1.46 in the (R)-MBCP-MMA system. Chiroptical properties of the polymers were also investigated. © 1992 John Wiley & Sons, Inc. 相似文献
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Shetnev A. A. Vasilieva E. A. Proskurina I. K. Forostyanko A. S. Presnukhina S. I. Tarasenko M. V. Lebedev A. S. Ivanovskii S. A. Kotov A. D. 《Russian Journal of Organic Chemistry》2022,58(3):306-314
Russian Journal of Organic Chemistry - A preparative procedure has been developed for the synthesis of a series of new medicinally relevant 3-aryl-5-(aryloxymethyl)-1,2,4-oxadiazoles in... 相似文献
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Leucine9-α-melanotropin ([Leu9]α-MSH) was synthesized in homogeneous solution by a fragment condensation approach, and it was assayed for its melanophore-dispersing and its tyrosinase-stimulating activity with a reflectometric in vitro frog skin assay and with cultured mouse melanoma cells, respectively. In both assay systems, parallel log dose-response curves were obtained for ([Leu9)]α-MSH and α-MSH; however, in the frog skin assay the activity of the title compound was 1 middot; 1010 Units/mmol, i.e. 25% of the activity of α-MSH, whereas its tyrosinasestimulating potency was only 1% compared to α-MSH (EC50= 2.5 · 10?7M ). This indicates a major difference in the recognition/stimulation process of the receptors of the two cell types. 相似文献
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P. A. Zoretic R. H. Khan M. L. Caspar M. D. Saltzman J. Jardin 《Journal of heterocyclic chemistry》1985,22(3):835-836
The synthesis of an oxotremorine analog, (E-5-oxo-2-(3α and 3β-hydroxy-1-octenyl)-1-(4-N-pyrrolidino-2-butynyl)pyrrolidine, is reported. 相似文献
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N'-5-四唑基-N-芳甲酰基硫脲的合成及其生物活性研究(I) 总被引:17,自引:0,他引:17
为寻找新的高活性农药,根据生物等排原理,设计合成了10种未见文献报道的 N'-5-(1H-1,2,3,4-四唑基)-N-芳甲酰基硫脲类化合物。它们的结构经IR,~1H NMR和元素分析确证。初步的生物活性测定结果表明,部分化合物具有优良的除草 活性或植物生长调节活性。 相似文献
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Tsutomu Oishi Kensoh Kagawa Minoru Fujimoto 《Journal of polymer science. Part A, Polymer chemistry》1995,33(8):1341-1352
Two types of optically active N-[N′-(α-methylbenzyl)amino/carbonyl-n-alkyl]maleimides (MBAC) were synthesized from maleic anhydride, 6-amino-n-caproic acid (or 12-amino-n-dodecanoic acid), and (R)-(+)-α-methylbenzylamine. Radical homopolymerizations of MBAC were performed in several solvents at 60 and 110°C for 24 h to give optically active polymers. Radical copolymerizations of MBAC were performed with styrene (ST) and methyl methacrylate (MMA) in dioxane at 60°C. The monomer reactivity ratios and the Alfrey-Price Q-e values were determined. Chiroptical properties of the polymers and copolymers were investigated. © 1995 John Wiley & Sons, Inc. 相似文献
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采用微波和相转移催化法通过1-苯基-5-(4-苯基-1,2,4-三唑-5-巯基-3-甲硫基)四唑(2)与2-氯乙酰芳胺(3)反应高效、快速地合成了10种尚未见文献报道的1-苯基-5-[5-(芳胺羰基甲硫基)-4-苯基-1,2,4-三唑-3-甲硫基]四唑. 其结构经 IR, 1H NMR, 13C NMR 和元素分析表征. 生物活性实验结果表明, 该类化合物在较低浓度下部分化合物对小麦芽有很好的促进作用. 相似文献
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1-芳酰基-4-(5-芳基-2-呋喃甲酰基)氨基硫脲衍生物的合成及其生物活性 总被引:11,自引:0,他引:11
酰胺基硫脲;芳基酰肼;1-芳酰基-4-(5-芳基-2-呋喃甲酰基)氨基硫脲衍生物的合成及其生物活性 相似文献
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A Schiff base was synthesized by 3-methyl-4-amino-5-ethoxycarbonyl-methylsulfanyl-1,2,4-triazole with 3-nitrobenzaldehyde. The structure was confirmed by 1H NMR, IR, H RMS, TGA techniques and X-ray diffraction. The crystal belongs to monoclinic system, space group P21/c, with a = 8.965(2), b = 21.903(5), c = 9.197(2) A, β = 114.011(4)°, C14H15N5O4 S, Mr = 349.08, V = 1649.7(6) A3, Dc = 1.407 g·cm-3, Z = 4, F(000) = 728, μ = 0.226 mm-1, the final R = 0.0574 and wR = 0.1336 for 2932 unique reflections with I 2σ(I). Furthermore, the biological activity to four vegetable pathogens has been tested. The title compound exhibits better biological activity to four vegetable pathogens compared to the Schiff base without 5-ethoxycarbonyl and to Gibberlla saubinetti in EC95 compared with triadimefon. 相似文献