Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca2+-activated K+ channels
作者:Donglai Yang、Lejla Arifhodzic、C. Robin Ganellin、Donald H. Jenkinson
DOI:10.1016/j.ejmech.2013.02.029
日期:2013.5
Previously, quinolinium-based tetraazacyclophanes, such as UCL 1684 and UCL 1848, have been shown to be extraordinarily sensitive to changes in chemical structure (especially to the size of the cyclophane system) with respect to activity as potent non-peptidic blockers of the small conductance Ca2+-activated K+ ion channels (SKCa). The present work has sought to optimize the structure of the linking
A cationic amphiphile for facilitating transport of a biologically active molecule into a cell has the structure A-F-D, in which A is a lipid anchor, D is a head group, and F is a spacer group having the structure described herein. A method for facilitating transport of a biologically active molecule into a cell comprises preparing a lipid mixture comprising a cationic amphiphile having structure A-F-D, preparing a lipoplex by contacting the lipid mixture with a biologically active molecule; and contacting the lipoplex with a cell, thereby facilitating transport of the biologically active molecule into the cell.
Design, synthesis and biological activity of peptidomimetic analogs of insect allatostatins
作者:Yong Xie、Zhen Peng Kai、Stephen S. Tobe、Xi Le Deng、Yun Ling、Xiao Qin Wu、Juan Huang、Li Zhang、Xin Ling Yang
DOI:10.1016/j.peptides.2010.10.016
日期:2011.3
punctata showed that the activity of analog I (IC(50): 0.09 muM) was more active than that of the C-terminal pentapeptide (Tyr-Xaa-Phe-Gly-Leu-NH(2), IC(50): 0.13 muM) it mimicked and the activity of the analog II (IC(50): 0.13 muM) proved roughly equivalent to the C-terminal pentapeptide. The results indicate that a new simple mimicry for Tyr-Xaa-Phe-Gly has been discovered; analog I may be a novel compound
Biphasic liquid/liquid reactions are commonplace, however their scale-up under super-heating conditions are not. An even more challenging effort has to be expected in case of a large scale continuous production...
Stereoelectronic Profiling of Expanded-Ring N-Heterocyclic Carbenes
作者:Anuj Kumar、Dan Yuan、Han Vinh Huynh
DOI:10.1021/acs.inorgchem.9b00786
日期:2019.6.3
Heterobis(carbene) complexes of palladium(II) and gold(I) containing expanded-ring N-heterocyclic carbenes (erNHCs) have been prepared in order to study their electronic properties. erNHCs with mesityl substituents were found to exhibit anisotropic interferences, which hampered ranking of their donicities by 13C NMR spectroscopy. The anisotropy effects were found to be stronger in the linear gold complexes
为了研究它们的电子性质,已经制备了含钯(II)和金(I)的带有杂环N-杂环卡宾(erNHCs)的杂双(卡宾)配合物。发现具有异氰酸酯取代基的erNHC表现出各向异性干扰,这妨碍了其13 C NMR光谱法对烯烃的排序。发现在线性金络合物中各向异性效应更强,其中较小的配位数使翼尖分散更多。具有柔性N-苄基的erNHC更合适,发现其供体强度从五元杂环逐渐增加到七元杂环。通过比较1 J也可以得到相同的趋势尽管无法检测到七元和八元erNHC之间的显着差异,但各个盐的(CH)耦合常数。从其钯和金配合物的结构获得的erNHC的%V bur值表明,各向异性干扰随着整体空间体积的增加而增加。