RESUMEN
Bromhexine is an expectorant drug repurposing as a TMPRSS2 inhibitor, which has also been proposed for potential treatment in COVID-19 infection. Multicomponent crystal strategy has been applied in bromhexine to improve its poor solubility, which limits its bioavailability and efficacy. A new bromhexine crystal and its fumarate salt crystal have been successfully obtained by slow evaporation technique. Both compounds have been characterized by X-ray single-crystal diffraction, TGA and FT-IR spectroscopy. Hirshfeld surface analysis has been carried out to further quantify the patterns of intermolecular interactions. Compared with bromhexine, the multicomponent crystal with pharmaceutically acceptable conformer of fumaric acid shows improved thermal stability and solubility in water.
RESUMEN
Hexafluoroisopropanol has been demonstrated as the versatile promoter for redox-neutral α-C(sp3)-H functionalization of cyclic amines via the cascade [1,5]-hydride transfer/cyclization strategy. A wide range of cyclic amines are functionalized into bioactive tetrahydroquinolines, quinazolines, benzoxazines, and benzotriazepines in moderate to excellent yields. This protocol features additive-free conditions, operational simplicity, and wide substrate scope.
RESUMEN
Erythropoietin-producing hepatomocellular receptors and their receptor-interacting proteins (Eph/ephrin) can participate in the regulation of growth and development and promote the development of diseases through short-distance signal transduction between cells. To study the mechanism of Eph/ephrin and oral-related diseases, we provided a new theoretical basis and a strategy for the treatment of oral diseases. The Eph/ephrin pathway has been used to regulate oral diseases, especially in periodontal disease prevention, orthodontic bone reconstruction, and biological treatment of oral tumors. This paper reviews the research progress of Eph/ephrin pathway in oral-related diseases.