Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives
F Chimenti1, B Bizzarri, F Manna
1Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università 'La Sapienza', P.le A. Moro 5, 00185 Rome, Italy.
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.
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