title: Synthesis and in vitro selective anti-Helicobacter pylori activity of N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides.
abstract: 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.
authors.affiliation: Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Chimenti
authors.forename: Bruna
authors.initials: B
authors.lastname: Bizzarri
authors.forename: Adriana
authors.initials: A
authors.lastname: Bolasco
authors.forename: Daniela
authors.initials: D
authors.lastname: Secci
authors.forename: Paola
authors.initials: P
authors.lastname: Chimenti
authors.forename: Simone
authors.initials: S
authors.lastname: Carradori
authors.forename: Arianna
authors.initials: A
authors.lastname: Granese
authors.forename: Daniela
authors.initials: D
authors.lastname: Rivanera
authors.forename: Daniela
authors.initials: D
authors.lastname: Lilli
authors.forename: M Maddalena
authors.initials: MM
authors.lastname: Scaltrito
authors.forename: M Immacolata
authors.initials: MI
authors.lastname: Brenciaglia
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D003374:Coumarins