%0 Journal Article
%T Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs
%J Pharmaceuticals | An Open Access Journal from MDPI
%D 2019
%R https://doi.org/10.3390/ph12020091
%X 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¨C16 ¦Ìg/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 ¡Ü 4 ¦Ìg/mL for 4c¨C 4h and 4k/ 4l) or E. coli (MIC = 32¨C64 ¦Ìg/mL for 4q¨C 4v) according to the global lipophilicity of these compounds. View Full-Tex
%U https://www.mdpi.com/1424-8247/12/2/91