- Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors
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H5N1 virus, one subtype of highly pathogenic influenza A virus in human infection, has recently received attention due to its unpredictable and high mortality. In this study, a series of arylsulfonamide derivatives were identified as improved H5N1 inhibitors for the influenza treatment by systematic structure-activity relationship investigation. Among them, the most potent H5N1 inhibitor 3h exhibited excellent antiviral activity against H5N1 virus with EC50 value of 0.006 μM and selectivity index 33543.3. Moreover, the molecular docking of 3h with M2 proton channel protein provides practical way for understanding the inhibition of H5N1 with this kind of compounds.
- Yu, Yongshi,Tang, Qi,Xu, Zhichao,Li, Siliang,Jin, Mengyu,Zhao, Zixuan,Dong, Chune,Wu, Shuwen,Zhou, Hai-Bing
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p. 206 - 216
(2018/10/15)
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- Nano-sized La0.5Ca0.5CoO3-mediated reduction by nabh4 of aryl nitriles to bis-(benzyl) amines
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Nano-sized La0.5Ca0.5CoO3 perovskite, which was produced via the sol-gel method, was an efficient heterogeneous catalyst in combination with NaBH4 for the rapid chemoselective reduction of aryl nitriles to bis-(benzyl)amines at 40°C in good to excellent yields. The physico-chemical properties of the catalyst were characterized by means of differential thermal analysis (DTA), thermogravimetric analysis (TGA), X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive spectroscopy (EDX) and particle size distributions images. The results show that nanoparticles have regular shapes with well-defined crystal faces with an average size of 30 nm.
- Bavandi, Hossein,Shiri, Ali,Tavakkoli, Haman
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p. 3330 - 3334
(2017/05/29)
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- Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: Comparison with effects on fatty acid amidohydrolase
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A new series of arachidonic acid derivatives were synthesized and evaluated as inhibitors of the endocannabinoid uptake. Most of them are able to inhibit anandamide uptake with IC50 values in the low micromolar range (IC50 = 0.8-24 μM). ln general, the compounds had only weak effects upon CB1, CB2, and VR1 receptors (Ki > 1000-10000 nM). In addition, there was no obvious relationship between the abilities of the compounds to affect anandamide uptake and to inhibit anandamide metabolism by fatty acid amidohydrolase (FAAH; IC50 = 30-113 μM). This indicates that the compounds do not exert their effects secondarily to FAAH inhibition. It is hoped that these compounds, particularly the most potent in this series (compound 5, UCM707, with IC50 values for anandamide uptake and FAAH of 0.8 and 30 μM, respectively), will provide useful tools for the elucidation of the role of the anandamide transporter system in vivo.
- López-Rodríguez, María L.,Viso, Alma,Ortega-Gutiérrez, Silvia,Fowler, Christopher J.,Tiger, Gunnar,De Lago, Eva,Fernández-Ruiz, Javier,Ramos, José A.
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p. 1512 - 1522
(2007/10/03)
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