RESUMEN
Polymer supported dichlorophosphate (PEG-OPOCl(2)) is an efficient green catalyst for the electrophilic substitution reaction of indole with aromatic aldehydes, in neat condition, to afford an excellent yield of bis(indolyl) methanes with short reaction time, at room temperature. The synthesized compounds and their anti-cancer activity are evaluated.
Asunto(s)
Antineoplásicos , Citotoxinas , Indoles , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Citotoxinas/síntesis química , Citotoxinas/química , Citotoxinas/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Indoles/síntesis química , Indoles/química , Indoles/farmacologíaRESUMEN
A series of α-hydroxyphosphonates were synthesized from the reaction of aldehyde (1) with triethylphosphite (2) in the presence of oxone and evaluated for their antioxidant properties against lipid peroxidation, reduced glutathione, superoxide dismutase, and catalase. The majority of the compounds showed promising antioxidant activity. Diethyl anthracen-9-yl (hydroxy) methylphosphonate (3n) is the most potent and biologically active compound against free radicals.
Asunto(s)
Antioxidantes/síntesis química , Diseño de Fármacos , Organofosfonatos/síntesis química , Animales , Antioxidantes/química , Antioxidantes/farmacología , Biomarcadores/análisis , Encéfalo/efectos de los fármacos , Encéfalo/enzimología , Encéfalo/metabolismo , Catalasa/metabolismo , Glutatión/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Estructura Molecular , Organofosfonatos/química , Organofosfonatos/farmacología , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismoRESUMEN
Sensorial analysis of pineapple breads (conventionally baked, Cpb; fully baked frozen, Fpb and partially baked, Ppb) showed no significant differences in terms of aroma and taste. On the contrary, the scores for the overall quality between the partially baked and conventionally baked breads showed significant (p < 0.05) differences. At the same time, headspace analysis using a solid-phase microextraction (SPME) method identified 59 volatile compounds. The results of the aroma extracts dilution analysis (AEDA) revealed 19 most odour-active compounds with FD factors in the range of 32-128 as the key odourants of the pineapple breads. Further analysis of the similarities and differences between the pineapple breads in terms of the key odourants were carried out by the application of PLS-DA and PLS-regression coefficients. Results showed that Ppb exhibited strong positive correlations with most of the volatile- and non-volatile compounds, while the Cpb showed significant positive correlations with hexanal and 4-hydroxy-2,5-dimethyl-3(2H)-furanone, and the Fpb had strong positive correlations with lactic acid, benzoic acid, benzaldehyde and ethyl propanoate.
Asunto(s)
Ananas/química , Análisis de los Alimentos , Cromatografía de Gases y Espectrometría de Masas/métodos , Odorantes/análisis , Microextracción en Fase Sólida/métodos , Benzaldehídos/análisis , Pan , Cromatografía de Gases , GustoRESUMEN
Synthesis of 1-substituted-1,3,2-diazaphosphole 1-oxides (3a-l) were accomplished via a two-step process. It involves the preparation of diazaphospholo 1-oxide monochloride intermediate (2) and its subsequent reaction with phenols/amino acid esters in dry THF in the presence of triethylamine at 40-45°C. The structures of newly synthesized compounds were characterized by spectral and elemental analysis. The title compounds were evaluated for their in-vitro antioxidant properties.