Stefano Rossetti

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF HYDROXYL-BISPHOSPHONIC ANALOGS OF BILE ACIDS

Bisphosphonates (BPs) are now the most widely used drugs for diseases associated with increased bone resorption, such as osteoporosis, and tumor bone diseases. A significant drawback of the BPs is their poor oral absorption that is enhanced by the presence of bile acid substituents in the bisphosphonate framework, with no toxic effects. A straightforward synthesis of bile acid-containing hydroxy-bisphosphonates and a full characterization of these pharmaceutically important molecules, including an evaluation of affinity and the mechanism of binding to hydroxyapatite, is presented. The biological activity of bile acid-containing bisphosphonate salts was determined using the neutral-red assay on the L929 cell line and primary cultures of osteoclasts. The bioactivity of the new compounds was found superior than bisphosphonates of established activity.

Selective removal of monoterpenes from bergamot oil by inclusion in deoxycholic acid.

A new approach for removing monoterpenes (MTs) from bergamot oil by selective inclusion in deoxycholic acid (DCA) is proposed. The inclusion process is very efficient, the included fraction being composed mainly of limonene (71.7%) and gamma-terpinene (19.8%). On the other hand, the deterpenated bergamot oil fraction showed for the linalool and linalyl acetate derivatives significant increases from 16.6 and 21.4% to 18.3 and 42.2%, respectively. The major advantages of this methodology are its simplicity, the mild conditions employed, and the quantitative recovery of both host (DCA) and guest (monoterpenes) compounds. Differential scanning calorimetry (DSC), thermal gravimetry (TG), powder X-ray diffractometry (XRPD), infrared spectroscopy (IR), and proton magnetic resonance ((1)H NMR) analysis were used to investigate and characterize the inclusion compounds.

Stabilization of tetrameric metavanadate ion by tris(1,10-phenanthroline)cobalt(III): Synthesis, spectroscopic and X-ray structural study of [Co(phen)(3)](3)(V(4)O(12))(2)Cl·27H(2)O.

A new complex salt of composition [Co(phen)3]3(V4O12)2Cl ⋅ 27H2O (phen = 1,10-phenanthroline and [V4O12]4− = tetrameric metavanadate, dodecaoxotetravanadate ion) was synthesized by the reaction of appropriate salts in aqueous medium. The complex salt has been characterized by elemental analyses, thermogravimetric analysis, cyclic voltammetry, FT-IR, and UV-Vis spectroscopies, solubility product and conductance measurements. Single crystal X-ray structure determination revealed ionic structure consisting of three complex cations, [Co(phen)3]3+, two [V4O12]4− anions, one chloride and 27 lattice water molecules. Detailed structural and spectroscopic analyses of [Co(phen)3]3(V4O12)2Cl ⋅ 27H2O showed that the large anion is stabilized by large cationic metal complex as there is preferred shape compatibility that leads to a large number of lattice-stabilizing non-covalent interactions.