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1.
Br Poult Sci ; : 1-6, 2019 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-30929462

RESUMEN

1. The effect of supplementing water-soluble vitamin E analogues 6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid (trolox) and butylated hydroxy toluene (BHT) was studied in two separate experiments. 2. In the first experiment, trolox was supplemented at 0.2 mM, 0.4 mM and 0.8 mM concentrations along with N-methylacetamide (MA; 12% final concentration) and semen was cryopreserved in 0.5 ml French straws. Different semen parameters and fertility were assessed from post-thaw samples. 3. Sperm motility, live sperm, and mitochondrial activity were significantly lower (P < 0.05) in cryopreserved semen. Lipid peroxidation (LPO) was significantly higher (P < 0.05) in cryopreserved semen that was reduced by trolox supplementation. The treatment containing trolox at 0.2 mM concentration produced significantly higher (P < 0.05) fertility compared to unsupplemented cryopreservation treatment. 4. In the second experiment, BHT was supplemented at 0.25 mM, 0.5 mM, and 1 mM concentrations along with MA during semen cryopreservation. 5. Sperm motility, live sperm and MTT dye reduction test were significantly lower (P < 0.05) in cryopreserved semen. These parameters declined with increasing BHT concentration. Abnormal sperm was significantly higher (P < 0.05) in the BHT supplemented treatments. The sperm chromatin dispersion (SCD) test was significantly higher (P < 0.05) in cryopreserved samples and was highest in samples supplemented with 0.5 mM and 1 mM BHT. The percentage fertility was significantly lower (P < 0.05) in cryopreserved semen and BHT supplementation did not improve fertility. 6. In conclusion, trolox supplementation at 0.2 mM concentration during semen cryopreservation improved fertility, whereas BHT supplementation resulted in a decline in post-thaw semen parameters.

2.
Bioorg Med Chem Lett ; 21(21): 6510-4, 2011 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-21924612

RESUMEN

Indole and its derivatives undergo smooth conjugate addition onto en-1,4-dione derived from isatin and acetophenone, in the presence of a catalytic amount of molecular iodine in acetonitrile under mild conditions to afford a novel class of 3-(1-(1H-indol-3-yl)-2-oxo-2-phenylethyl)indolin-2-one derivatives in good yields with high degree of 1,4-selectivity. Some of these compounds are found to exhibit modest antibacterial and antifungal properties.


Asunto(s)
Antibacterianos/química , Antifúngicos/química , Indoles/química , Yodo/química , Antibacterianos/farmacología , Antifúngicos/farmacología , Catálisis , Yodo/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja
3.
Bioorg Med Chem Lett ; 21(13): 3890-3, 2011 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-21641208

RESUMEN

A simple and efficient synthetic approach toward a series of chiral aryl boronate esters, starting from D-xylose, as anti-microbial agents, is described herein. Minimum inhibitory concentration and zone of inhibition revealed that these derivatives exhibit potent anti-bacterial and anti-fungal properties. Herein, we report the first anti-microbial activity of this class of compounds. All products have been characterized by NMR ((1)H, (13)C and (11)B), IR, elemental and mass spectral study.


Asunto(s)
Antibacterianos , Antifúngicos , Bacterias/efectos de los fármacos , Ésteres/síntesis química , Ésteres/farmacología , Hongos/efectos de los fármacos , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/síntesis química , Antifúngicos/química , Antifúngicos/farmacología , Boratos/síntesis química , Boratos/química , Boratos/farmacología , Ésteres/química , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad , Xilosa/síntesis química , Xilosa/química , Xilosa/farmacología
4.
Eur J Med Chem ; 45(1): 78-84, 2010 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-19931223

RESUMEN

The formation of N- and O-propargylated quinazoline derivatives 2, 3 from quinazol-4-ones 1 was theoretically predicted by optimizations at B3LYP/6-31G* level, analysed kinetically and thermodynamically. Theoretical predictions are validated by experiment to observe the trends and found deviation. Thus, compound 1 was propargylated in basic media to obtain compound 2 and 3 in definite proportions. Each compound was further subjected to [3+2] cycloaddition using perfluoroalkyl azides through Click reaction under Sharpless conditions, and obtained a series of novel perfluoroalkyl-1H,1,2,3-triazol-4-yl substituted quinazolines 4, 5, and 6. All the compounds were screened for antimicrobial activity and identified potential compounds.


Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Quinazolinas/química , Quinazolinas/farmacología , Triazoles/química , Antiinfecciosos/síntesis química , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Conformación Molecular , Quinazolinas/síntesis química , Reproducibilidad de los Resultados , Termodinámica
5.
J Enzyme Inhib Med Chem ; 24(2): 559-65, 2009 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-18951276

RESUMEN

A versatile and efficient method has been developed for the synthesis of bis(indolyl)methanes by using aluminium triflate (0.5 mol%) as a novel catalyst. Further, some of the synthesized compounds were evaluated for their efficacy as antibacterial and antifungal activities. Most of the compounds have shown moderate to good inhibitory activity.


Asunto(s)
Antibacterianos/síntesis química , Indoles/síntesis química , Metano/química , Antibacterianos/farmacología , Catálisis , Indoles/farmacología , Metano/análogos & derivados , Metano/farmacología , Pruebas de Sensibilidad Microbiana
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