Decavanadate salts with nicotinamide (3-pyridinecarboxamide, 3-pca) and isonicotinamide (4-pyridinecarboxamide, 4-pca) in both neutral and protonated forms, (3-Hpca)[HVO]·2HO·2(3-pca) (complex I) and (4-Hpca)[HVO]·2(4-pca) (complex II), have been synthesized and characterized by vibrational spectroscopy (infrared and Raman), thermogravimetric analysis (TGA), V NMR, and single-crystal X-ray diffraction analysis. The effects of sodium decavanadate (henceforth called NaV) and compounds I and II on Escherichia coli, Giardia intestinalis, and Vero (African green monkey epithelial kidney) cells were evaluated. Enhanced growth inhibitory activity against E. coli cultures was observed upon treatment with products I and II when compared to that with NaV (GI values of 2.8, 4.0, and 11 mmol L, respectively), as well as lower cell viability as measured by the intake of propidium iodide (PI). Exposure of Giardia trophozoites to NaV and II revealed reduction in trophozoite viability (GI values of ca. 10 μmol L) and affected the parasite adherence to both polystyrene culture tubes and a monolayer of Vero cells, even at low concentrations. A lesser effect on Giardia was shown for I. Furthermore, all three compounds were significantly less toxic to Vero cells than the reference drug, albendazole, employed in the treatment of giardiasis. Toxicity reports of oxidovanadium compounds toward Giardia are unprecedented and open a path to the development of new therapeutic agents.
The solid-state investigation
of the diastereomeric salts (S)-ibuprofen (S-Ibu),
(S)-naproxen, (S-Nap),
and (S)-ketoprofen (S-Ket) with (R)-(+)- and (S)-(−)-1-phenylethylamine, R-PEA,
and S-PEA respectively, has been carried out by using a combination
of experimental and in-silico tools. The focus was
on their crystal packing and on the stability/transformation of their
solid forms under different experimental conditions with the final
aim of extracting useful information on the forces/features which
could be exploited for the chiral separation of the corresponding
racemic compounds. All the salts are 21-column crystals,
each column consisting of API and 1-phenylethylamine ions assembled
via the 1-phenylethylammonium-carboxylate supramolecular heterosynthon
which originates a R
4
3 (10) pattern, the intercolumns contacts being
definitely weaker. In spite of an overall similarity in the crystal
packing forces and motifs of the anhydrous salts, the temperature
stability range suggests that the homochiral species are the most
stable. The fact that the homochiral salt of S-Ket (S-Ket_S-PEA) is stable toward the hydration, at variance with the heterochiral
one (S-Ket_R-PEA), further confirms this hypothesis.
On the other hand, preliminary sorption tests show that S-Ket and
S-Ibu preferentially capture the homochiral PEA (S-Nap is not selective).
This behavior has been correlated to the almost planar boundary surfaces
which characterize and differentiate the 21 sheets in S-Ket_S-PEA and S-Ibu_S-PEA salts with respect
to the corresponding heterochiral ones.
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