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MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate
- Source :
-
Bioorganic & Medicinal Chemistry . Nov2007, Vol. 15 Issue 22, p7087-7097. 11p. - Publication Year :
- 2007
-
Abstract
- Abstract: A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, substituted at the 2-position with piperidines bearing quaternary ammonium salt side chains, were synthesized and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the β-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Attachment of the charged entity using an N-ethylcarbamoyloxy linker led to the discovery of the highly soluble compound 22 (D13-9001), which maintained good potency in vitro and displayed excellent activity in vivo in a rat pneumonia model of P. aeruginosa. [Copyright &y& Elsevier]
- Subjects :
- *PSEUDOMONAS aeruginosa
*PSEUDOMONAS
*PYROMEN
*PSEUDOMONADACEAE
Subjects
Details
- Language :
- English
- ISSN :
- 09680896
- Volume :
- 15
- Issue :
- 22
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26863007
- Full Text :
- https://doi.org/10.1016/j.bmc.2007.07.039