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 lg/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.
A novel class of selective anti-Helicobacter pylori agents 2-Oxo-2H-chromene-3-carboxamide derivatives / Chimenti, Franco; Bizzarri, Bruna; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Carradori, Simone; Granese, Arianna; Rivanera, Daniela; Lilli, Daniela; Zicari, Alessandra; SCALTRITO M., M; Sisto, F.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 17(11):(2007), pp. 3065-3071. [10.1016/j.bmcl.2007.03.050]
A novel class of selective anti-Helicobacter pylori agents 2-Oxo-2H-chromene-3-carboxamide derivatives.
CHIMENTI, Franco;BIZZARRI, Bruna;BOLASCO, Adriana;SECCI, DANIELA;CHIMENTI, Paola;CARRADORI, Simone;GRANESE, ARIANNA;RIVANERA, Daniela;LILLI, Daniela;ZICARI, Alessandra;
2007
Abstract
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 lg/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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
