This paper describes an efficient approach for the synthesis of a novel series of sixteen 2-(5-trifluoromethyl-1H-pyrazol-1-yl)-5-(5-trihalomethyl-1H-pyrazol-1-yl-1-carbonyl) pyridines, for the first time with non-identical substituents in both pyrazole rings, through the cyclocondensation reaction of 4-methoxy-4-alkyl(aryl/heteroaryl-1,1,1-trihaloalk-3-en-2-ones [CX3C(O)CH=CR1OCH3, in which R1 = CH3, C6H5, 4-CH3C6H4, 4-OCH3C6H4, 2-furyl and X = F, Cl] or acetylacetone with some 6-[3-alkyl(aryl)-5-trifluoromethyl-1H-pyrazol-1-yl]nicotinohydrazides. Optimized yields of 67-91% were obtained when the reactions were performed in ethanol (green solvent) at reflux for 16 h. Subsequent antioxidant and antimicrobial evaluation revealed promising 1,1-diphenyl-2-picrylhydrazyl (DPPH) inhibition percentage and exhibited fungiostatic and fungicidal activities against yeasts, dermatophytes and filamentous, especially for the pyridine systems, when the both pyrazole rings attached to a pyridine ring contain CX3 groups (X = H, F, Cl) of different kinds. It is also observed the trichloromethyl substituted compounds presented higher antioxidant activity in comparison to their fluorinated analogous.

The aim of this work was to test the hypothesis that a moderate intake of organic purple grape juice shows a positive radiomodifier effect over early behavioural damage following acute X-irradiation in mice. Anxiety-, locomotion-, and feeding-related responses to 6 Gy total body X-irradiation (TBI) were studied via open field, Rotarod, and feeding/drinking recording. Thirty-two male mice weighing 25-30 g were grouped according grape juice (J) or water (W) ad libitum drinking and either non-irradiated (N) or irradiated (R). 24 h post-TBI the access frequency to the center and corners of the open field was decreased, and the total stay in the corners increased, in RW vs. NW mice. Anxiety-related parameters decreased in RJ vs. RW mice. Rotarod latency times increased 72 h post-TBI in RJ vs RW mice. No overall changes in food and drink intake were observed along the experimental period. On the irradiation day, bout number was increased and bout duration was decreased in RW mice. The changes were reversed by purple grape juice intake. Grape juice intake before and after TBI can overcome several radiation-induced changes in behaviour within 24-72 hours after sub-lethal X-irradiation. This beneficial effect on short-term anxiety and mobility-related activities could probably be included in the list of flavonoid bio-effects. The present findings could be relevant in designing preventive interventions aimed to enhance body defense mechanisms against short-term irradiation damage.

El presente estudio tiene como objetivo comprobar la hipótesis de que una ingesta moderada de mosto ecológico de uva tinta presenta un efecto radiomodificador positivo sobre los daños comportamentales tempranos inducidos por la irradiación aguda con rayos X en el ratón. Se estudiaron respuestas relacionadas con el comportamiento ingestivo, ansiedad y locomoción frente a la irradiación aguda a cuerpo entero (TBI) con 6 Gy de rayos X, mediante registro directo de la ingestión de agua y alimento, rotarod y open field. Se utilizaron 32 ratones macho con un peso corporal entre 25 y 30 g, agrupados en función de haber sido sometidos a irradiación a cuerpo entero (R) o no (N) y de su ingesta de mosto (J) o agua (W) ad libitum. La frecuencia de acceso al centro y a las esquinas del open field disminuyó 24 horas después de la irradiación, mientras que aumentó la duración de la estancia en las esquinas en los ratones RW respecto a los NW. Los parámetros relacionados con ansiedad disminuyeron en ratones RJ respecto a los RW. No se observaron cambios significativos en la ingestión total de alimento y bebida durante los días analizados; sin embargo, en el día de la irradiación disminuyó el número total de episodios ingestivos al tiempo que aumentó el tamaño de los mismos. Estos cambios revirtieron en los animales que bebieron mosto. La ingesta de mosto antes y después de la irradiación puede revertir cambios comportamentales agudos inducidos por la irradiación subletal. El efecto beneficioso sobre la ansiedad y actividad motora a corto plazo podría ser relevante para diseñar intervenciones preventivas encaminadas a incrementar los mecanismos de defensa del cuerpo frente al daño por irradiación a corto plazo.