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 μg/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 / F. Chimenti, B. Bizzarri, A. Bolasco, D. Secci, P. Chimenti, S. Carradori, A. Granese, D. Rivanera, D. Lilli, A. Zicari, M.M. Scaltrito, F. Sisto. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 17:11(2007 Jun), pp. 3065-3071.
A novel class of selective anti-Helicobacter pylori agents 2-oxo-2H -chromene-3-carboxamide derivatives
M.M. ScaltritoPenultimo
;F. SistoUltimo
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 μg/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.Pubblicazioni consigliate
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