In this work, we present the physicochemical characterization and structural determination of two sulfonylhydrazone derivatives: LASSBio-1773 and LASSBio-1774. The former compound has displayed hypoglycemic activity and has reduced the thermal hyperalgesia and mechanical allodynia in a murine model of diabetic neuropathic pain induced by streptozotocin. In order to stablish the differences in the three-dimensional characteristics of these original bioactive compounds, we determined their crystal structures-by using X-ray powder diffraction data and a simulated annealing procedure-and studied their thermal stability. Furthermore, we performed crystal morphology prediction and compared it with SEM photomicrographs: the evidenced good agreement allowed us to suggest alternative crystallization routes-to overcome the low-solubility of LASSBio-1773 and LASSBio-1774-as evidenced by IDR tests
Structural and physicochemical characterization of some sulfonylhydrazone derivatives designed as hypoglycemic agents
Punzo F.;
2017-01-01
Abstract
In this work, we present the physicochemical characterization and structural determination of two sulfonylhydrazone derivatives: LASSBio-1773 and LASSBio-1774. The former compound has displayed hypoglycemic activity and has reduced the thermal hyperalgesia and mechanical allodynia in a murine model of diabetic neuropathic pain induced by streptozotocin. In order to stablish the differences in the three-dimensional characteristics of these original bioactive compounds, we determined their crystal structures-by using X-ray powder diffraction data and a simulated annealing procedure-and studied their thermal stability. Furthermore, we performed crystal morphology prediction and compared it with SEM photomicrographs: the evidenced good agreement allowed us to suggest alternative crystallization routes-to overcome the low-solubility of LASSBio-1773 and LASSBio-1774-as evidenced by IDR testsFile | Dimensione | Formato | |
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