66 research outputs found
âLantern-Shapedâ Platinum(III) Complexes with Axially Bound 9-Ethylguanine or 1-Methylcytosine (L) of General Formula [Pt2{HN=C(But)O}4L2](NO3)2
The synthesis, NMR characterization, and X-ray crystallography of âlantern-shapedâ platinum(III) complexes with four pivaloamidate bridging ligands and two 9-ethylguanines (9-EtG) or 1-methylcytosines (1-MeC) in axial positions are reported: cis-N2O2-[Pt2{HN=C(But)O}4(9-EtG)2](NO3)2 and cis-N2O2-[Pt2{HN=C(But)O}4(1-MeC)2](NO3)2. The last complex is, to the best of our knowledge, the first dinuclear compound of platinum(III) with axially bound 1-MeC
2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers
Enantiomeric forms of Tocainide, Mexiletine, and structurally related local anaesthetic compounds, were
analyzed with respect to their potency in blocking Nav1.4 channel. Structureâactivity relationships based
on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular
surface as well as the presence of specific polar spacers might be determinant for receptor interactions.
QSAR and pharmacophore models were then used to support at 3D level this hypothesisEnantiomeric forms of Tocainide. Mexiletine, and structurally related local anaesthetic compounds, were analyzed with respect to their potency in blocking Na(v)1.4 channel. Structure-activity relationships based on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular surface as well as the presence of specific polar spacers might be determinant for receptor interactions. QSAR and pharmacophore models were then used to support at 3D level this hypothesis. (C) 2008 Elsevier Masson SAS. All rights reserved
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