0000000000750011
AUTHOR
María Teresa Albelda
Protonation, coordination chemistry, cyanometallate "supercomplex" formation and fluorescence chemosensing properties of a bis(2,2'-bipyridino)cyclophane receptor.
A new polyazamacrocycle (L) containing two 2,2'-bipyridino (bpy) units, where the heteroaromatic nitrogen atoms point outwards from the macrocyclic cavity, was synthesized and characterized by elemental analysis, ESI-MS, (1)H and (13)C NMR, FTIR and TGA. Five protonation constants involving aliphatic nitrogens with log K in the range 9.39-3.07 were determined by potentiometry and NMR and a sixth protonation (log K = 2.2) involving a bipyridine moiety could be detected by UV-Vis and NMR titrations. The interaction of L with the cyanometallate anions [Pt(CN)4](2-) and [Co(CN)6](3-) was studied by potentiometry yielding respectively log K values in the ranges 4.0-6.4 and 5.2-10.5, covering pro…
Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids.
SUMMARYThe synthesis and antiprotozoal activity of some simple dialkyl pyrazole-3,5-dicarboxylates (compounds 2–6) and their sodium salts (pyrazolates) (compounds 7–9) against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis are reported. In most cases the studied compounds showed, especially against the clinically significant amastigote forms, in vitro activities higher than those of the reference drugs (benznidazole for T. cruzi and glucantime for Leishmania spp.); furthermore, the low non-specific cytotoxicities against Vero cells and macrophages shown by these compounds led to good selectivity indexes, which are 8–72 times higher for T. cruzi amastigotes and 15–113 tim…
Nanoparticles as Contrast Agents for MRI of Atherosclerotic Lesions
Nanoparticle contrast agents for MRI may aid in identifying atherosclerotic lesions that give rise to ischemic events by means of penetration and retention in the plaque. These imaging agents may provide valuable information regarding plaque characteristics which can help determine the risk of plaque rupture. By increasing molecular flexibility or adding a means of specifically targeting ligands via antibody or peptide, nanoparticles can enhance certain regions of the atherosclerotic plaque. The development of single contrast agents detectable with multiple imaging modalities may further improve our ability to detect and characterize atherosclerosis in clinical and preclinical applications.…
CRT-605 Multimodality Imaging Demonstrating Liposomes Preferentially Home to Regions of Myocardial Injury
Nanoparticles may serve as a promising means to deliver novel therapeutics to the myocardium following myocardial infarction. We assessed whether lipid-based liposomal nanoparticles specifically target injured myocardium following intravenous injection. CD1 male mice that underwent LAD ligation