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S-Monofluoromethyl phosphorothioates represent an important class of organofluorine compounds and are re ported here for the first time.A series of S-monofluoromethyl phosphorothioates are conveniently synthesized from different PⅤ-H compounds and PhSO2SCH2F under mild conditions.The method is compatible with common functional groups and provides potential opportunities to synthesize new bioactive molecules for medicinal chemistry. 相似文献
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袁文腾 《电信工程技术与标准化》2004,(9):18-21
本文介绍了中国联通青岛分公司为提高CDMA网络质量、提高网络维护效率,开发并投入使用的一套话务统计与实时报警软件(CAS)。 相似文献
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Nomeir AA Pramanik BN Heimark L Bennett F Veals J Bartner P Hilbert M Saksena A McNamara P Girijavallabhan V Ganguly AK Lovey R Pike R Wang H Liu YT Kumari P Korfmacher W Lin CC Cacciapuoti A Loebenberg D Hare R Miller G Pickett C 《Journal of mass spectrometry : JMS》2008,43(4):509-517
Posaconazole (SCH 56592) is a novel triazole antifungal drug that is marketed in Europe and the United States under the trade name 'Noxafil' for prophylaxis against invasive fungal infections. SCH 56592 was discovered as a possible active metabolite of SCH 51048, an earlier lead. Initial studies have shown that serum concentrations determined by a microbiological assay were higher than those determined by HPLC from animals dosed with SCH 51048. Subsequently, several animals species were dosed with (3)H-SCH 51048 and the serum was analyzed for total radioactivity, SCH 51048 concentration and antifungal activity. The antifungal activity was higher than that expected based on SCH 51048 serum concentrations, confirming the presence of active metabolite(s). Metabolite profiling of serum samples at selected time intervals pinpointed the peak that was suspected to be the active metabolite. Consequently, (3)H-SCH 51048 was administered to a large group of mice, the serum was harvested and the metabolite was isolated by extraction and semipreparative HPLC. LC-MS/MS analysis suggested that the active metabolite is a secondary alcohol with the hydroxyl group in the aliphatic side chain of SCH 51048. All corresponding monohydroxylated diastereomeric mixtures were synthesized and characterized. The HPLC retention time and LC-MS/MS spectra of the diastereomeric secondary alcohols of SCH 51048 were similar to those of the isolated active metabolite. Finally, all corresponding individual monohydroxylated diasteriomers were synthesized and evaluated for in vitro and in vivo antifungal potencies, as well as pharmacokinetics. SCH 56592 emerged as the candidate with the best overall profile. 相似文献
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Masahiko Isaka Somporn PalasarnSomjit Komwijit Sayanh SomrithipolSujinda Sommai 《Tetrahedron letters》2014
Cyclodepsipeptides SCH 217048 (1), SCH 218157 (2), and a new analog, pleosporin A (3), were isolated from cultures of an unidentified elephant dung fungus of the family Pleosporaceae. The structure of 3 was elucidated on the basis of detailed spectroscopic interpretation. The absolute configurations of 1–3 were determined by chiral column HPLC analysis and Marfey’s method. Cyclodepsipeptides 1–3 exhibited antimalarial activity against Plasmodium falciparum K1 with respective IC50 values of 1.6, 6.4, and 1.6 μg/mL, while they did not show cytotoxicity against KB, MCF-7 and NCI-H187 cell-lines or non-cancerous Vero cells at 50 μg/mL. 相似文献
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Justin Tatch Moore 《Annals of Pure and Applied Logic》2006,140(1-3):128-132
The purpose of this paper is to present some results which suggest that the Singular Cardinals Hypothesis follows from the Proper Forcing Axiom. What will be proved is that a form of simultaneous reflection follows from the Set Mapping Reflection Principle, a consequence of PFA. While the results fall short of showing that MRP implies SCH, it will be shown that MRP implies that if SCH fails first at κ then every stationary subset of reflects. It will also be demonstrated that MRP always fails in a generic extension by Prikry forcing. 相似文献
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《Analytical letters》2012,45(7):1335-1344
Abstract A rapid method is described for the determination of SCH 29482. This is based on the spectrophotometric measurement at 386 nm of the product of reaction with imidazole formed at 35°Cin a 1.5 M imidazole and 2×10?3M mercuric chloride solution at pH 7.50. The method, which permits detection of concentrations of SCH 29482 as low as to 2.8, μg/ml, is reproducible and specific for intact SCH 29482 in the presence of degradation products. The molar absorptivity for the chromophore formed is 2.54×l04 I mol?1cm?1. 相似文献
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