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Bioorg Med Chem Lett ; 15(3): 603-7, 2005 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-15664821

RESUMEN

In order to develop new anti-Helicobacter pylori agents, a series of N1-substituted 3,5-diphenyl pyrazolines P1-P13 was prepared and evaluated for their antibacterial activity. All synthesized compounds showed little or no activity against different species of Gram-positive and Gram-negative bacteria of clinical relevance and against various strains of pathogenic fungi. The same derivatives exhibited a significant degree of activity against a range of H. pylori strains, including those resistant to the reference compound metronidazole. Among the prepared compounds those with an N1-acetyl group and a 4-methoxy substituent in the 5-phenyl ring showed the best activity against H. pylori metronidazole resistant strains in the 1-4 microg/mL MIC range.


Asunto(s)
Antibacterianos/síntesis química , Helicobacter pylori/efectos de los fármacos , Pirazoles/síntesis química , Antibacterianos/farmacología , Resistencia a Medicamentos , Humanos , Metronidazol , Pruebas de Sensibilidad Microbiana , Pirazoles/farmacología , Especificidad de la Especie , Relación Estructura-Actividad
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