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51.
Structure-activity relationships of a new antifungal imidazole, AFK-108, and related compounds 总被引:1,自引:0,他引:1
Hori K Sakaguchi A Kudoh M Ishida K Aoyama Y Yoshida Y 《Chemical & pharmaceutical bulletin》2000,48(1):60-64
Fungicidal activity of widely used imidazole antifungal drugs in topical applications is not so strong in spite of their fungistatic activities against dermatophytes and pathogenic yeasts. In order to improve fungicidal activity of imidazole antifungal agents, a series of novel imidazole derivatives having a hydrophobic substituent derived from isoprenoid were synthesized. The efficacy of these compounds was evaluated with respect to direct cell-membrane damaging activity, ergosterol biosynthesis inhibition, minimum growth-inhibitory concentration (MIC) and therapeutic effect for experimental dermatophytosis of guinea pigs. Among the newly synthesized compounds, the geranyl derivative named AFK-108 (2a) showed the highest in vivo fungicidal activity with both cell membrane damaging activity and ergosterol biosynthesis inhibition in vitro. 相似文献
52.
Makoto Minato Takefumi Kaneko Shogo Masauji Takashi Ito 《Journal of organometallic chemistry》2006,691(11):2483-2488
We describe the synthesis of a new asymmetric P,N,N′-tridentate ligand (bis(pyrid-2-ylethyl) menthylphosphine, BPEMP), containing two pyridyl rings and (1S,2R,5S)-menthylphosphino group. The ligand is obtained in five steps from natural abundant l-menthol. The coordination behavior of the ligand toward cationic (allylic)Pd(II) moiety and its first application in palladium-catalyzed asymmetric allylic alkylation are presented. Crystallographic and spectroscopic analyses reveal that [(η3-allylic)Pd(BPEMP)]+ complex forms only one isomer in the solid state as well as in solution. 相似文献
53.
A highly convergent total synthesis of gymnocin-A, a cyctotoxic polyether marine natural product, has been achieved. The synthesis features Suzuki-Miyaura coupling of the ABCD and FGHIJKLMN rings, stereoselective introduction of the C17 hydroxyl group, ring-closure of the F ring, and a late-stage incorporation of a 2-methyl-2-butenal side chain. 相似文献
54.
Post-biotinylation of the alkyl azide derivative of trifluoromethyl phenyldiazirine (TPD) was elucidated to apply a photoaffinity biotinylation technique. A photo-modified polyvinilidene difluoride (PVDF) membrane was used as a photolabeled component and we introduced biotin by Staudinger-Bertozzi ligation. The 15 pmol amount of biotinylated reagent was still effective for the visualization of cross-linked product on the matrix. The results show the potential utility of alkyl azide carrying TPD derivatives in the application of photoaffinity biotinylation, which could be useful for the ligands with tight structural requirements. 相似文献
55.
Takeo Miyazawa Takeshi Endo Makoto Okawara 《Journal of polymer science. Part A, Polymer chemistry》1985,23(5):1527-1535
Some hindered amine polymers containing 2,2,6,6-tetramethylpiperidine structure were synthesized. A new monomer, 4-O-vinylbenzyl-2,2,6,6-tetramethylpiperidine, was homopolymerized and copolymerized with some vinyl monomers in the presence of AIBN as an initiator. The obtained amine polymers were oxidized with hydrogen peroxide to obtain the polymers having nitroxyl radical moiety. 相似文献
56.
Fumiyo Saito Ryo Takeuchi Tomoyuki Kamino Kouji Kuramochi Kengo Sakaguchi Susumu Kobayashi Masashi Tsuda 《Tetrahedron letters》2004,45(43):8069-8071
A total synthesis of the proposed structure of plakevulin A was accomplished. However, the NMR spectral data of the synthetic plakevulin A were not identical of those of the reported compound. We next converted the synthetic plakevulin A into 1-dihydrountenone A. The 1H and 13C NMR spectral data of 1-dihydrountenone A were identical with those of reported plakevulin A except for the peaks derived from levulinic acid. Thus, we repurified sample of the natural product and confirmed that the natural sample contained 1-dihydrountenone A and levulinic acid in the ratio of one to one. We also found that not plakevulin A but 1-dihydountenone A possessed the inhibitory activity against mammalian DNA polymerases α and β. 相似文献
57.
Homogeneous solutions are formed from equimolar amounts of Ce(NH4)2(NO3)6 and EDTA. These solutions hydrolyze single-stranded DNA far more efficiently than double-stranded DNA. In contrast, Ce(IV) hydroxide gel, obtained in the absence of EDTA, hydrolyzes both single-stranded and double-stranded DNAs at almost the same rates. In order to achieve this substrate-specificity sufficiently, the mole ratio of EDTA to Ce(NH4)2(NO3)6 must be 1.0 or greater. By using this remarkable specificity of Ce(IV)/EDTA complex, gap-site in substrate DNA is selectively hydrolyzed. The scission-site is modulated by use of appropriate combination of oligonucleotide additives. The reactions have been kinetically analyzed. 相似文献
58.
De-Qi Yuan Yuewei Zhao Makoto Fukudome Kahee Fujita 《Journal of inclusion phenomena and macrocyclic chemistry》2007,57(1-4):125-129
One or two coumarin units were incorporated to the primary face of γ-cyclodextrin (γ-CD), and the resultant coumarin derivatives
were employed to harvest the chemical energy generated in the reaction of bis(trichlorophenyl)oxalate with hydrogen peroxide.
In comparison with the coumarin without CD cavity for molecular recognition, the coumarin–CD conjugates demonstrated much
higher chemiluminescence inetensity, indicating that the CD moiety remarkably improves the chemical energy transfer. 相似文献
59.
Yoshizawa M Ono K Kumazawa K Kato T Fujita M 《Journal of the American Chemical Society》2005,127(31):10800-10801
Two molecules of planar MII(acac)2 complexes (M = Pt, Pd, and, Cu; acac = acetylacetonato) are efficiently stacked within an organic-pillared coordination cage, exhibiting characteristic spectroscopies (for M = Pt and Pd) and electron spin-spin coupling (for M = Cu) attributable to metal-metal interaction. 相似文献
60.
A series of parallel reactions were carried out for the tandem Ugi/Diels-Alder reaction on our MPEG-O-CH2- platform. Ninety-six out of a 100 entries were successful to give complex heterotricycles. The stereoselectivity was found not to be influenced by the building blocks used for amine and carboxylic acid components. An unexpected side pathway was found but was suppressed by employing appropriate reaction conditions. The reaction was also performed on solid phase, by which a larger library is potentially realized by employing the split-pool method. 相似文献