RESUMEN
Twenty benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety were synthesized and evaluated for their anti-oxidant and anti-inflammatory activities. Among these compounds, 8h and 8l were appeared to have high radical scavenging efficacies as 0.05 ± 0.02 and 0.07 ± 0.03 mmol/L of IC50 values in ABTS+ bioassay, respectively. In anti-inflammatory tests, compound 8h displayed good activity with 57.35% inhibition after intraperitoneal administration, which was more potent than the reference drug (indomethacin). Molecular modeling studies were performed to investigate the binding mode of the representative compound 8h into COX-2 enzyme. In vitro enzyme study implied that compound 8h exerted its anti-inflammatory activity through COX-2 inhibition.
Asunto(s)
Antiinflamatorios/uso terapéutico , Benzotiazoles/uso terapéutico , Depuradores de Radicales Libres/uso terapéutico , Inflamación/tratamiento farmacológico , Oxadiazoles/uso terapéutico , Animales , Antiinflamatorios/síntesis química , Antiinflamatorios/metabolismo , Benzotiazoles/síntesis química , Benzotiazoles/metabolismo , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2/síntesis química , Inhibidores de la Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2/uso terapéutico , Depuradores de Radicales Libres/síntesis química , Depuradores de Radicales Libres/metabolismo , Humanos , Ratones , Simulación del Acoplamiento Molecular , Estructura Molecular , Oxadiazoles/síntesis química , Oxadiazoles/metabolismo , Relación Estructura-ActividadRESUMEN
Myopia is one of the three main school public health problems in China, the prevalence of which has been showing a rising and low-aging tendency in the past few decades. High myopia can cause several vision -threatening problems such as degenerative retinal conditions, cataracts, retinal detachment, and choroidal neovascularization. Its related complications are the leading causes of visual impairment and blindness, adversely impacting the afflicted individual's quality of life. Therefore, the prevention and control of myopia have become a common concern of family, school and health department. The purpose of this review is to summarize the progression of a variety of intervention methods used to prevent and control childhood myopia in recent years.
RESUMEN
On the basis of high binding affinity of 2-hexynyl-N(6)-methyladenosine and N(6)-substituted-4'-thioadenosine derivatives at the A3 adenosine receptor (AR), novel 2-alkynyl-substituted-N(6)-methyl-4'-thioadenosine derivatives, combining the characteristics of two classes of nucleosides were designed and synthesized from D-gulonic gamma-lactone via palladium-catalyzed cross coupling reaction as a key step. Among compounds tested, only compound 3b showed moderate binding affinity at the human A3 adenosine receptor without binding affinities at other subtypes.
Asunto(s)
Adenosina/análogos & derivados , Receptores Purinérgicos P1/metabolismo , Tionucleósidos/síntesis química , Adenosina/síntesis química , Adenosina/metabolismo , Animales , Células CHO , Catálisis , Cricetinae , Cricetulus , Diseño de Fármacos , Humanos , Indicadores y Reactivos , Espectroscopía de Resonancia Magnética , Paladio , Espectrofotometría Ultravioleta , Tionucleósidos/metabolismoRESUMEN
In view of biological activities of tiazofurin and azido or aminosugar nucleosides, novel azido- and amino-substituted tiazofurin derivatives (1 and 2) were efficiently synthesized starting from 1,2;5,6-di-O-isopropylidene-D-glucose.