Next Article in Journal
CDK8-Novel Therapeutic Opportunities
Previous Article in Journal
Novel 11-Substituted Ellipticines as Potent Anticancer Agents with Divergent Activity against Cancer Cells
Previous Article in Special Issue
De Novo Design and In Vitro Testing of Antimicrobial Peptides against Gram-Negative Bacteria
Article Menu
Issue 2 (June) cover image

Export Article

Open AccessArticle

Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs

AGIR, EA 4294, UFR of Pharmacy, Jules Verne University of Picardie, 80037 Amiens, France
Department of Bacteriology, Amiens University Hospital, 80054 Amiens, France
Respiratory and Intensive Care Unit, University Hospital Amiens, 80054 Amiens, France
Authors to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(2), 91;
Received: 29 May 2019 / Revised: 12 June 2019 / Accepted: 14 June 2019 / Published: 18 June 2019
PDF [1732 KB, uploaded 20 June 2019]


The lack of antibiotics with a novel mode of action associated with the spread of drug resistant bacteria make the fight against infectious diseases particularly challenging. A quinoline core is found in several anti-infectious drugs, such as mefloquine and bedaquiline. Two main objectives were set in this work. Firstly, we evaluated the anti-mycobacterial properties of the previous quinolines 3, which have been identified as good candidates against ESKAPEE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp. and Escherichia coli) bacteria. Secondly, a new series 4 was designed and assessed against the same bacteria strains, taking the pair of enantiomers 3m/3n as the lead. More than twenty compounds 4 were prepared through a five-step asymmetric synthesis with good enantiomeric excesses (>90%). Interestingly, all compounds of series 3 were efficient on M. avium with MIC = 2–16 µg/mL, while series 4 was less active. Both series 3 and 4 were generally more active than mefloquine against the ESKAPEE bacteria. The quinolines 4 were either active against Gram-positive bacteria (MIC ≤ 4 µg/mL for 4c4h and 4k/4l) or E. coli (MIC = 32–64 µg/mL for 4q4v) according to the global lipophilicity of these compounds. View Full-Text
Keywords: Quinoline; tuberculosis; nosocomial infections; ESKAPEE bacteria; mycobacterium Quinoline; tuberculosis; nosocomial infections; ESKAPEE bacteria; mycobacterium

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material


Share & Cite This Article

MDPI and ACS Style

Laumaillé, P.; Dassonville-Klimpt, A.; Peltier, F.; Mullié, C.; Andréjak, C.; Da-Nascimento, S.; Castelain, S.; Sonnet, P. Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs. Pharmaceuticals 2019, 12, 91.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top