Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs

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...

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Vydané v:	Pharmaceuticals Ročník 12; číslo 2; s. 91
Hlavní autori:	Laumaillé, Pierre, Dassonville-Klimpt, Alexandra, Peltier, François, Mullié, Catherine, Andréjak, Claire, Da-Nascimento, Sophie, Castelain, Sandrine, Sonnet, Pascal
Médium:	Journal Article
Jazyk:	English
Vydavateľské údaje:	Switzerland MDPI AG 18.06.2019 MDPI
Edícia:	Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry
Predmet:	[CHIM]Chemical Sciences [SDV]Life Sciences [q-bio] Antibiotics Antimicrobial agents Bacteria Chemical Sciences Drugs E coli ESKAPEE bacteria Gram-negative bacteria Gram-positive bacteria Infectious diseases Life Sciences Medicine mycobacterium Nosocomial infections Pathogens Pharmacy and materia medica Quinoline R RS1-441 Staphylococcus infections Tuberculosis Quinoline mycobacterium nosocomial infections ESKAPEE bacteria tuberculosis
ISSN:	1424-8247, 1424-8247
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Shrnutí:	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 4c–4h and 4k/4l) or E. coli (MIC = 32–64 µg/mL for 4q–4v) according to the global lipophilicity of these compounds.
Bibliografia:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 14 content type line 23 PMCID: PMC6630482
ISSN:	1424-8247 1424-8247
DOI:	10.3390/ph12020091