A series of new 2-phenyl-quinoline-4-carboxylic acid derivatives was synthesized starting from aniline, 2-nitrobenzaldehyde, pyruvic acid followed by Doebner reaction, amidation, reduction, acylation and amination. All of the newly-synthesized compounds were characterized by 1H-NMR, 13C-NMR and HRMS. The antibacterial activities of these
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A series of new 2-phenyl-quinoline-4-carboxylic acid derivatives was synthesized starting from aniline, 2-nitrobenzaldehyde, pyruvic acid followed by Doebner reaction, amidation, reduction, acylation and amination. All of the newly-synthesized compounds were characterized by
1H-NMR,
13C-NMR and HRMS. The antibacterial activities of these compounds against Gram-negative (
Escherichia coli,
Pseudomonas aeruginosa) and Gram-positive bacteria (
Staphylococcus aureus,
Bacillus subtilis), as well as one strain of methicillin-resistant
Staphylococcus aureus (MRSA) bacteria were evaluated by the agar diffusion method (zone of inhibition) and a broth dilution method (minimum inhibitory concentration (MIC)), and their structure-activity relationships were obtained and discussed. The results revealed that some compounds displayed good antibacterial activity against
Staphylococcus aureus, and Compounds 5a
4 and 5a
7 showed the best inhibition with an MIC value of 64 μg/mL against
Staphylococcus aureus and with an MIC value of 128 μg/mL against
Escherichia coli, respectively. The results of the MTT assay illustrated the low cytotoxicity of Compound 5a
4.
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