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Molecules 2016, 21(3), 340; doi:10.3390/molecules21030340

Design, Synthesis and Antibacterial Evaluation of Some New 2-Phenyl-quinoline-4-carboxylic Acid Derivatives

1
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China
2
Department of Hematology, Donghua Affiliated Hospital of Sun Yat-sen University, Dongguan 523110, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 24 January 2016 / Revised: 19 February 2016 / Accepted: 7 March 2016 / Published: 10 March 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [464 KB, uploaded 15 March 2016]   |  

Abstract

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 5a4 and 5a7 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 5a4. View Full-Text
Keywords: 2-phenyl-quinoline-4-carboxylic acid derivatives; synthesis; Doebner reaction; antibacterial activity 2-phenyl-quinoline-4-carboxylic acid derivatives; synthesis; Doebner reaction; antibacterial activity
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Wang, X.; Xie, X.; Cai, Y.; Yang, X.; Li, J.; Li, Y.; Chen, W.; He, M. Design, Synthesis and Antibacterial Evaluation of Some New 2-Phenyl-quinoline-4-carboxylic Acid Derivatives. Molecules 2016, 21, 340.

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