Artículos de revistas
Understanding the solid forms of 5E-phenylethenylbenzofuroxan with different in vivo anti-T. cruzi activity
Fecha
2013-11Registro en:
Revista Virtual de Química, Niterói : Sociedade Brasileira de Química - SBQ, v. 5, n. 6, p. 1179-1190, Nov. 2013
1984-6835
Autor
Honorato, Sara B.
Porcal, Williams
Merlino, Alicia
Ellena, Javier
Cerecetto, Hugo
Ayala, Alejandro P.
González, Mercedes
Institución
Resumen
5E-Phenylethenylbenzofuroxan (5PhEBfx) was reported as an excellent anti-Chagas drug candidate. However, its oral bioavailability was affected by the crystallization process. Two samples exhibiting variable in vivo activity was investigated: a thin yellow powder (5PhEBfx-Y) and orange needles (5PhEBfx-O). X-ray powder diffraction, differential scanning calorimetry, vibrational spectroscopy, optical and electron scanning microscopies were applied to investigate both solid forms in order to correlate the solid-state properties with the variable bioavailability of 5PhEBfx. It was observed that 5PhEBfx-Y have a better solubility and consequently higher bioavailability when compared with 5PhEBfx-O. This result suggests that the difference of activity between these two 5E-Phenylethenylbenzofuroxanes could be associated with the solid forms, which also cause the coloration variation.