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Coimbra, Portugal

E. Castro R.A.,CEF | Ribeiro J.D.B.,CQC | Maria T.M.R.,CQC | Ramos Silva M.,University of Coimbra | And 3 more authors.
Crystal Growth and Design | Year: 2011

A screening of naproxen cocrystals with coformers picolinamide, nicotinamide, isonicotinamide, and pyrazinamide is performed by the Kofler contact method and mechanochemistry. The solids obtained by mechanochemistry are characterized by differential scanning calorimetry, DSC, polarized light thermomicroscopy, PLTM, infrared spectroscopy, FTIR, and X-ray powder diffraction, XRPD. No cocrystal could be prepared under the experimental conditions investigated between naproxen and pyrazinamide, which bears two aromatic nitrogen atoms, ortho and meta to the amide group. For the o-, m-, and p-pyridinecarboxamide isomers, regardless of the aromatic nitrogen position, the coformer interacts with naproxen to give rise to new cocrystals: naproxen:picolinamide, naproxen2:nicotinamide, and naproxen:isonicotinamide. A supramolecular acid:aromatic nitrogen heterosynthon is found in all these cocrystals. The structure of the new naproxen: isonicotinamide compound was solved by single-crystal X-ray diffraction, SXD. As nicotinamide has FDA/GRAS status the naproxen:nicotinamide (2:1) cocrystal is of special relevance. © 2011 American Chemical Society.

Simoes A.V.C.,CQC | Pinto S.M.A.,CQC | Calvete M.J.F.,CQC | Gomes C.M.F.,University of Coimbra | And 5 more authors.
RSC Advances | Year: 2015

Herein we report, for the first time, the development, labeling optimization and preliminary biodistribution studies of an [18F] radiolabeled meso-tetraphenylporphyrin. After synthesis and characterization of the "cold" fluorinated porphyrin, the conditions have been transferred to an automated radiochemistry module and the desired 5-(2-[18F]fluoroethoxyphenyl)-10,15,20-triphenylporphyrin was prepared in a radiochemical purity >95%. Moreover, data regarding the uptake into human bladder tumor cells and the radiotracer biodistribution after C57BL/6 mice injection are also presented. The maximum cellular uptake was reached at 45 min and was of 2.5%. © 2015 The Royal Society of Chemistry.

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