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Bioorg Med Chem Lett ; 15(3): 603-7, 2005 Feb 01.
Article in English | MEDLINE | ID: mdl-15664821

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Helicobacter pylori/drug effects , Pyrazoles/chemical synthesis , Anti-Bacterial Agents/pharmacology , Drug Resistance , Humans , Metronidazole , Microbial Sensitivity Tests , Pyrazoles/pharmacology , Species Specificity , Structure-Activity Relationship
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