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191.
Eman M. Flefel Waled A. Tantawy Randa E. Abdel-Mageid Abd El-Galil E. Amr Rolla Nadeem 《Research on Chemical Intermediates》2014,40(4):1365-1381
3-(Naphthalen-1-ylmethylene)-5-phenylfuran-2(3H)-one 1 was prepared and converted into a variety of heterocyclic systems of synthetic and biological importance. Benzylamine was reacted with furanone 1 to afford compounds 2 and 3 according to the reaction conditions. Butanamide 2 was reacted with thionyl chloride or thiourea to give derivatives 4 and 5, respectively. Compound 3 was reacted with ethyl cyanoacetate to give the corresponding pyrrolopyridine derivative 6. Treatment of 1 with hydrazine hydrate afforded compounds 7 and 8 according to the reaction conditions. Also, compound 1 was reacted with phenyl hydrazine, hydroxyl amine, malononitrile or thiourea to give compounds 9–12, respectively. Cyclization of 7 with ethoxymethylene-malononitrile, ethyl-(ethoxymethylene)cyanoacetate, carbon disulphide or acetylacetone afforded the corresponding compounds 13–16, respectively. Condensation of 7 with p-nitrobenzaldehyde gave the corresponding hydrazone 17, which was treated with thioglycolic acid or chloroacetyl chloride to give compounds 18 and 19, respectively. Also, most of the prepared products were tested for anti-avian influenza virus and revealed promising antiviral activity against H5N1 virus [A/Chicken/Egypt/1/2006 (H5N1)] by determination of both TC 50 and ED 50 and confirmed by plaque reduction assay on MDCK cells. Compounds 7, 8, 11, 12 and 13 showed the highest effect compared with the other tested compounds. 相似文献
192.
Paraoxonase-1 (PON-1) is a high-density-lipoprotein-bound enzyme, and its major function is to prevent oxidation of low-density
lipoprotein. Atherogenesis could be related to decreased activity of this enzyme. Nitrites (), either present as a contaminant and/or the main metabolic end product of nitric oxide (NO) degradation, may trigger nitrative
damage to PON-1 enzyme. Minimal information is available concerning the effect of nitrite on the enzyme activity and the mechanism
which it exerts its effect. The aim of this study was to analyze whether nitrites could play a role in modifying human PON-1
activity. Our results revealed that PON-1 activity was inhibited by nitrite in dose- and time-dependent manner. Site-specific
nitration focused on phenolic residues, particularly tyrosine residues of the enzyme, may result in modification of its biological
functions. Nitration of phenolic residues occurs via peroxynitrite (ONOO−) formation, which requires peroxides and nitrite. Thus, we tested the presence of peroxides, which are found in all plasma
samples regardless of nitrite concentration. The inhibition of PON-1 activity by nitrite was significantly reduced by tryptophan,
reduced glutathione (GSH), and catalase additions. Therefore, we concluded that nitrites may have a role in the inactivation
of PON-1, probably through nitration of enzyme phenyl residues, and additions of individual aromatic amino acids, with highlighting
on tryptophan, could be of important value in minimizing the nitrite-induced inhibition of PON-1 enzyme. 相似文献
193.
Billye Cheek Mieczyslaw Dabkowski Amr El Nagdi Louis R. Hunt T. P. LaFaveJr Ke Liu Duncan L. MacFarlane Viswanath Ramakrishna 《Acta Appl Math》2012,118(1):107-123
In this work, we consider design questions for an active optical lattice filter, which is being manufactured at the University
of Texas at Dallas, and which has proven to be useful in the signal processing task of RF channelization. The filter can be
described by a linear, discrete time state space model. The controlling agents, the gains, are embedded in the matrices intervening
in this state space model. Consequently, techniques from linear feedback control theory do not apply. We concentrate on the
question of finding real valued gains so that the A matrix of the state space model has a prescribed characteristic polynomial. We find that three of the coefficients can be
arbitrarily picked, but that the remaining are constrained by these and the other system parameters. Our techniques use methods
from constructive algebraic geometry. 相似文献
194.
Joan J. Soldevila-Barreda Andrea Pettenuzzo Maria Azmanova Laia Rafols Amr A. A. Attia Alexandru Lupan Luca Ronconi Nicolas P. E. Barry Anaïs Pitto-Barry 《Helvetica chimica acta》2023,106(8):e202300064
The synthesis by transmetallation and in-depth characterisation by IR spectroscopy of five half-sandwich ruthenium and osmium dithiocarbamato isonipecotamide glycoconjugate complexes are presented herein. The evaluation of their in vitro cytotoxicity and of the zinc precursors’ in vitro cytotoxicity towards ovarian cancer (A2780 and A2780cisR) and normal prostate (PNT2) cells is reported. While the cytotoxicity of the compounds is rather limited, some selectivity is observed. 相似文献