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991.
992.
Mario Merslavič Branko Stanovnik Miha Tišler 《Monatshefte für Chemie / Chemical Monthly》1985,116(12):1447-1458
New syntheses of oxazolo[4,5—d]pyridazine derivatives7 and11 were achieved by the cyclization of substituted N-pyridazin-5-ylformamide oximes6 and10. Under mild reaction conditions the transformations of the substituted amino group at position 2 of the oxazolo[4,5—d]pyridazine system7 occured to produce the compounds11, 14, and15, while under more drastic reaction conditions the nucleophilic attack at carbon at position 2 followed by the ring opening of the oxazole part of the molecule was observed to give the compounds13, 16, 17 and18.
Transformationen von N-Heteroarylformamidinen und N-Heteroarylformamidinoximen. Neue Synthesen und Transformationen von Oxazolo[4,5—d]pyridazinen
Zusammenfassung Mittels Cyclisierung substituierter N-Pyridazin-5-ylformamidoxime6 und10 wurden neue Synthesemöglichkeiten von Oxazolo[4,5—d]pyridazinderivaten erschlossen. Bei milden Reaktionsbedingungen trat Transformation der substituierten Aminogruppe an Position 2 des Oxazolo[4,5—d]pyridazin-Systems unter Bildung der Verbindungen11, 14 und15 ein, währenddessen unter drastischeren Reaktionsbedingungen ein nucleophiler Angriff am Kohlenstoff-2, gefolgt von einer Ringöffnung unter Bildung der Verbindungen13, 16, 17 und18 eintrat.相似文献
993.
P. C. Gopalratnam N. S. Mason R. E. Sparks 《Applied biochemistry and biotechnology》1984,10(1-3):213-220
Schistosomiasis is among the top five diseases in the world in terms of morbidity, affecting perhaps 200 million people in
tropical and subtropical countries. Antischistosomal drugs are toxic and rapidly metabolized. Hence, they must be given in
a number of spaced doses. In spite of this there are severe side effects leading to poor patient compliance. This is an ideal
situation for the application of sustained drug release to avoid the toxic peak concentration of drug.
This study was carried out using Astiban acid, an antimonial drug that is effective againstS. mansoni. Unfortunately, the drug is sufficiently soluble that 50 mg will dissolve in 100 mL water in less than a minute. To permit
sustained release of intramuscularly injected drug, microcapsules of astiban acid in poly(d,l-lactic acid) were formed by coacervation.
Release studies show that an appreciable fraction of the drug is available at the surface for rapid solution. After this surface
drug dissolves, the remaining drug is released slowly with half-times of many hours. After the initial burst, the release
of drug follows Higuchi’s equation up to approximately 80% release, with exponentially decreasing release rates thereafter. 相似文献
994.
The homogeneous phase Nb6I11?xBrx (0 ? x ? 2.7) is synthesized from Nb3Br8, Nb3I8 and Nb in sealed Nb capsules at 1 130 K. A second-order phase transition is found as for the composition Nb6I11 itself, changing the space group from P21cn (low temperatures) to Pccn, accompanied by a spin-crossover from a doublet to a quartet state. With increasing Br content the lattice constants decrease and the transition temperature shifts from 274 to 170 K while the transition interval is broadened simultaneously. Single crystal investigations for x = 0.5 and 2.3, each at 110 and 298 K, indicate a preferred substitution of one of the bridging I positions (I6) by Br atoms. 相似文献
995.
Moldovan Z Stoica C Hillebrand M Alexandrescu L Macovescu G 《Analytical and bioanalytical chemistry》2005,381(7):1381-1386
Phenyl--naphthylamine (PBN) used as rubber antioxidant was found to have native fluorescence. A spectrofluorimetric method for determination of PBN in multicomponent mixtures of polymer additives is described. The apparent excitation and fluorescence wavelengths used are 348 and 413.5 nm, respectively. Maximum fluorescence intensity is obtained by irradiating PBN dissolved in ethanol, at room temperature. The fluorescence varies linearly with the concentration of PBN in the range of 0.04–4 g mL–1. The accuracy and precision of the method are reported. 相似文献
996.
The racemization of d ‐aspartic acid to l ‐aspartic acid has been successfully performed with a coupled enzyme system at 90 °C and a pH of about 4.0 by the assay of high‐performance liquid chromatography. This coupled enzymatic racemization is a successive two‐step reaction first induced by d ‐amino acid oxidase and a subsequent coupled reaction by an aminotransferase clonezyme with the help of coenzyme pyridoxal 5′‐phosphate and cosubstrate l ‐glutamate. Due to the very high temperature, part of the l ‐aspartic acid is produced by the thermal effect. In fact the thermal racemization for aspartic acid can proceed from either d ‐ or l ‐aspartic acid via an intermediate fumaric acid and leads to the formation of d ,l ‐malic acid. The formation of α‐oxalacetic acid formed irreversibly from d ‐aspartic acid with d ‐amino acid oxidase can induce a side reaction to l ‐alanine. The thermal effect may also be responsible for the production of d ‐, and l ‐alanine. 相似文献
997.
The frequency shifts of the O-H stretching modes and the resonance components R of these shifts in the IR spectra of H-complexes of phenol with thiophene derivatives having organic and organosilicon substituents have been analyzed. Relationship of and R parameters to values calculated by nonempirical methods that characterize the electronic effect of organic substituents on the effective charges of the thiophene ring atoms has been established. It has been shown that in the complexation of phenol (hard acid) with thiophene derivatives charge control prevails over frontier orbital control. The changes in the effective charges of the thiophene ring atoms due to the effect of organosilicon substituents have been calculated.For the previous publication of this series see Ref. 1.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 12, pp. 2163–2168, December, 1994.This work was supported by the Russian Foundation for Basic Research, Project No. 93-03-18725. 相似文献
998.
In this paper, the variational inverse method for determining the depth of nonhomogeneous surface layers in elastic materials, from the measurements of the group velocity of surface shear horizontal (SH) waves, is developed. The direct problem for a given a priori type of profile of the coefficientc44in(x) (e.g. linear, Gaussian, etc.) is solved. The dispersion curves of phase and group velocity of surface SH waves in nonhomogeneous solids are calculated. Experimental verification of the inverse method has been performed for step profiles (structure of Cu on steel). It is stated that the inverse method based on the measurements of group velocity (for step profile) gives a smaller error in the unknown depth of the surface layer than that resulting from the inverse method based on the measurements of phase velocity of surface SH waves. 相似文献
999.
《Arabian Journal of Chemistry》2022,15(4):103720
Graviola, soursop, or guanabana (Annona muricata L.), is an ethnomedical fruit consumed to alleviate headache, diarrhea, diabetes, and cancer. Pericarp is the inedible part of graviola least studied in comparison to seeds and leaves, even thought, it contains the highest concentration of graviola total polyphenols. Anticancer effect of graviola pericarp has been demonstrated in crude extracts attributing the effect to acetogenins, however, crude extracts contain several active molecules. Thus, the present work aimed to fractionate and purify an ethanolic crude extract from graviola pericarp. Purified graviola pericarp fraction (PGPF) was evaluated on cancerous and non-cancerous cell lines, and then was identified by NMR, TOF-MS, and HPLC. Finally, an in silico analysis was performed to predict targets cancer-related of the molecule detected. Our results revealed IC50 values for cervix adenocarcinoma (HeLa), hepatocellular carcinoma (HepG2), triple-negative breast cancer (MDA-MB-231), and non-cancerous cell line (HaCaT) of 92.85 ± 1.23, 81.70 ± 1.09, 84.28 ± 1.08, and 170.2 ± 1.12 µg PGPF/mL, respectively. In vitro therapeutic indexes estimated as quantitative relationship between safety and efficacy of PGPF were 1.83, 2.08, and 2.02 for HeLa, HepG2, and MDA-MB-231, respectively. The NMR analysis revealed astragalin (kaempferol-3-O-glucoside) in PGPF, a flavonoid not reported in graviola pericarp until now. Astragalin identity was confirmed by TOF-MS and HPLC. In silico results support previous reports about astragalin modulating proteins such as Bcl-2, CDK2, CDK4, MAPK and RAF1. Also, results suggest that astragalin may interact with other cancer-related proteins not associated previously with astragalin. In conclusion, astragalin may be contributing to the anticancer effect observed in graviola pericarp extracts. 相似文献
1000.
Didier Degout Fayez Kassabji Pierre Fauchais 《Plasma Chemistry and Plasma Processing》1984,4(3):179-198
After a review of the literature on titanium production under plasma conditions, the main parameters controlling the reactions
(residence time, type and relative quantity of reducer, reaction temperature, etc.) are emphasized. The controlled-atmosphere
chamber where the rutile or anatase particles are heated and partly reduced in a crucible by a d.c. plasma torch with Ar-H2 as plasma gas is described. Study of the temperature dependence of the Gibbs free energy allows one to explain, at least
qualitatively, the experimental results obtained which correspond at best to 10% (weight) of TiO2 reduced to TiO by carbon. 相似文献