RESUMEN
The aim of this work is to improve the solubility and bioavailability of chlortetracycline and the function of the immune response. Chlortetracycline bisulfate and chlortetracycline mesylate were successfully synthesized and characterized with several techniques, including spectroscopy, chromatography and mass spectrometry, which demonstrated that the C4-dimethylamino group of chlortetracycline can accept a proton from sulfuric acid and methanesulfonic acid to form the corresponding salts. In addition, chlortetracycline bisulfate and chlortetracycline mesylate were more soluble in water than chlortetracycline hydrochloride, but the antibacterial activity was not enhanced. The influences of chlortetracycline hydrochloride, chlortetracycline bisulfate and chlortetracycline mesylate on chlortetracycline and immunoglobulin concentrations in mouse serum were also investigated. These results suggested that the chlortetracycline bisulfate and chlortetracycline mesylate have good bioavailability and strong immune response and have potential applications in animal breeding and formulation technologies.
Asunto(s)
Antibacterianos/química , Clortetraciclina/química , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacocinética , Bacterias/efectos de los fármacos , Disponibilidad Biológica , Clortetraciclina/síntesis química , Clortetraciclina/farmacocinética , Inmunidad Celular/efectos de los fármacos , Inmunoglobulinas/análisis , Mesilatos , Ratones , Pruebas de Sensibilidad Microbiana , Solubilidad , SulfatosRESUMEN
Guided by a "chemistry first" approach using molecular networking, eight new bright-blue colored natural compounds, namely dactylocyanines A-Hâ (3-10), were isolated from the Polynesian marine sponge Dactylospongia metachromia. Starting from ilimaquinoneâ (1), an hemisynthetic phishing probe (2) was prepared for annotating and matching structurally related natural substances in D.â metachromia crude extract network. This strategy allowed characterizing for the first time in Nature the blue zwitterionic quinonoid chromophore. The solvatochromic properties of the latter are reported.
Asunto(s)
Clortetraciclina/análogos & derivados , Poríferos/química , Animales , Productos Biológicos/síntesis química , Productos Biológicos/química , Productos Biológicos/aislamiento & purificación , Clortetraciclina/síntesis química , Clortetraciclina/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Cristalografía por Rayos X , Espectroscopía de Resonancia Magnética , Conformación Molecular , Poríferos/metabolismo , Quinonas/química , Sesquiterpenos/química , Espectrometría de Masas en TándemRESUMEN
The undecose nucleoside antibiotics herbicidin C and aureonuclemycin are biologically highly active and represent challenging targets for total synthesis. Herein, the gradual evolution of our synthetic strategy toward these natural products is described in detail. The initial route encompasses metalate addition chemistry but suffers from poor stereochemical control. In contrast, the ultimately successful strategy benefits from a variety of reagent-controlled stereoselective transformations, including a surprisingly facile and highly diastereoselective N-glycosylation process. The presented work also describes new building blocks that might find further application in carbohydrate chemistry.
Asunto(s)
Adenosina/análogos & derivados , Productos Biológicos/química , Productos Biológicos/síntesis química , Clortetraciclina/química , Clortetraciclina/síntesis química , Compuestos Heterocíclicos con 3 Anillos/química , Compuestos Heterocíclicos con 3 Anillos/síntesis química , Nucleósidos/química , Nucleósidos/síntesis química , Adenosina/síntesis química , Adenosina/química , Antibacterianos/síntesis química , Glicosilación , EstereoisomerismoRESUMEN
Better late than never! Two herbicidins, members of an important family of nucleoside antibiotics, have been synthesized for the first time. The route integrates a stereoselective C-glycosylation with several reagent-controlled stereoselective transformations and a surprisingly facile and highly diastereoselective late-stage N-glycosylation.
Asunto(s)
Adenosina/análogos & derivados , Antibacterianos/síntesis química , Clortetraciclina/análogos & derivados , Clortetraciclina/síntesis química , Compuestos Heterocíclicos con 3 Anillos/síntesis química , Nucleósidos de Purina/síntesis química , Adenosina/síntesis química , Glicosilación , Modelos Moleculares , Estructura Molecular , EstereoisomerismoRESUMEN
Varius classes of organic compounds, such as acids, aldehydes, ketones, alcohols and others getting into the atmosphere and polluting it were determined in the effluent gases of chlortetracycline production with chemical and physico-chemical methods.