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 ?g/ml MIC range, indicating the presence of an acyl function as an important feature for activity
Synthesis and in vitro selective anti-Helicobacter pylori activity of N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides / Chimenti, Franco; Bizzarri, Bruna; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Carradori, Simone; Granese, Arianna; Rivanera, Daniela; Lilli, Daniela; Maddalena Scaltrito, M.; Immacolata Brenciaglia, M.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 41:2(2006), pp. 208-212. [10.1016/j.ejmech.2005.11.001]
Synthesis and in vitro selective anti-Helicobacter pylori activity of N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides
Franco Chimenti;Bruna Bizzarri;Adriana Bolasco;Daniela Secci;Paola Chimenti;Simone Carradori;Arianna Granese;Daniela Rivanera;Daniela Lilli;
2006
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 ?g/ml MIC range, indicating the presence of an acyl function as an important feature for activityI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
