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.
Synthesis and In Vitro Selective anti-Helicobacter pylori Activity of Pyrazoline Derivatives / Chimenti, Franco; Bizzarri, Bruna; Manna, Fedele; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Granese, Arianna; Rivanera, Daniela; Lilli, Daniela; M. M., Scaltrito; M. I., Brenciaglia. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 15(3):(2005), pp. 603-607. [10.1016/j.bmcl.2004.11.042]
Synthesis and In Vitro Selective anti-Helicobacter pylori Activity of Pyrazoline Derivatives
CHIMENTI, Franco;BIZZARRI, Bruna;MANNA, Fedele;BOLASCO, Adriana;SECCI, DANIELA;CHIMENTI, Paola;GRANESE, ARIANNA;RIVANERA, Daniela;LILLI, Daniela;
2005
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.