Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives.
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.
Chimenti
F
F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università 'La Sapienza', P.le A. Moro 5, 00185 Rome, Italy.
Bizzarri
B
B
Manna
F
F
Bolasco
A
A
Secci
D
D
Chimenti
P
P
Granese
A
A
Rivanera
D
D
Lilli
D
D
Scaltrito
M M
MM
Brenciaglia
M I
MI
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004351:Drug Resistance; D016480:Helicobacter pylori / Q000187:drug effects*; D006801:Humans; D008795:Metronidazole; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013045:Species Specificity; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D011720:Pyrazoles; D008795:Metronidazole