Synthesis and in vitro selective anti-Helicobacter pylori activity of N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides.
In order to develop new anti-Helicobacter pylori agents, five new and three already known N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides (coumarin-3-carboxamides) were 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. Among the prepared compounds those with a 4-acyl-phenyl group showed the best activity against H. pylori metronidazole resistant strains in the 0.25-1 microg/ml MIC range, indicating the presence of an acyl function as an important feature for activity.
Chimenti
Franco
F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
Bizzarri
Bruna
B
Bolasco
Adriana
A
Secci
Daniela
D
Chimenti
Paola
P
Carradori
Simone
S
Granese
Arianna
A
Rivanera
Daniela
D
Lilli
Daniela
D
Scaltrito
M Maddalena
MM
Brenciaglia
M Immacolata
MI
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D024881:Drug Resistance, Bacterial; D016480:Helicobacter pylori / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests
D000900:Anti-Bacterial Agents; D003374:Coumarins