A novel class of selective anti-Helicobacter pylori agents 2-oxo-2H-chromene-3-carboxamide derivatives.
A novel class of selective anti-Helicobacter pylori agents, 2-oxo-2H-chromene-3-carboxamide derivatives, were prepared and evaluated for their anti-bacterial activity. All synthesized compounds showed little or no activity against different species of Gram-positive and Gram-negative bacteria and against various strains of pathogenic fungi. Some of them exhibited a potent and specific inhibitory effect on the growth of H. pylori, including metronidazole-resistant strains, in the 0.0039-16 microg/mL MIC range. A cytotoxic screening by the Trypan blue dye exclusion assay was also carried out on the most active compounds as anti-H. pylori agents. Among the derivatives examined for their cytotoxic potential, a number of them induced low cytotoxic effects.
Chimenti
Franco
F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, P.le A. 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
Zicari
Alessandra
A
Scaltrito
M Maddalena
MM
Sisto
Francesca
F
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis*; D005658:Fungi / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016480:Helicobacter pylori / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D010648:Phenylacetates / Q000138:chemical synthesis*; D014343:Trypan Blue / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D001578:Benzopyrans; D010648:Phenylacetates; D014343:Trypan Blue