Anti- Helicobacter pylori activities of selected N -substituted cinnamamide derivatives evaluated on reference and clinical bacterial strains

JOURNAL OF ANTIBIOTICS(2018)

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摘要
In this study, thirty-five N -substituted derivatives of cinnamic acid amide (cinnamamide) were evaluated for anti- Helicobacter pylori activity using an agar disc-diffusion method. Qualitative screening was performed on a reference H. pylori strain (ATCC 43504), resulting in the identification of the three most active compounds, 8 ( R,S -(2 E )-3-(4-chlorophenyl)- N -(2-hydroxypropyl)prop-2-enamide, minimal inhibitory concentration, MIC = 7.5 µg/mL), 23 ((2 E )-3-(4-chlorophenyl)- N -(2-hydroxycyclohexyl)prop-2-enamide, MIC = 10 µg/mL), and 28 ((2 E )-3-(4-chlorophenyl)- N -(4-oxocyclohexyl)prop-2-enamide, MIC = 10 µg/mL). These compounds were further tested on twelve well-characterized clinical strains, yielding MIC values that ranged from 10 to 1000 µg/mL. Preliminary safety assessments of the compounds were made using the MTT viability test for cytotoxicity and Ames test for mutagenicity, which showed them to be generally safe, although compounds 8 and 28 showed mutagenic activity at some of the tested concentrations. The results of this study showed the anti- H. pylori potential of cinnamamide derivatives.
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关键词
Drug development,Drug discovery and development,Life Sciences,general,Microbiology,Medicinal Chemistry,Organic Chemistry,Bacteriology,Bioorganic Chemistry
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