Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosa.
Several classes of peptidomimetics of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02,595) have been prepared and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin in Pseudomonas aeruginosa. A number of the new analogues were as active or more active than the lead, demonstrating that a peptide backbone is not essential for activity.
Renau
Thomas E
TE
Essential Therapeutics, Inc., 850Maude Avenue, Mountain View, CA 94043, USA. trenau@etrx.com
Léger
Roger
R
Yen
Rose
R
She
Miles W
MW
Flamme
Eric M
EM
Sangalang
Joan
J
Gannon
Carla L
CL
Chamberland
Suzanne
S
Lomovskaya
Olga
O
Lee
Ving J
VJ
D000890:Anti-Infective Agents / Q000494:pharmacology*; D001693:Biological Transport, Active / Q000187:drug effects; D004357:Drug Synergism; D064704:Levofloxacin; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors*; D008826:Microbial Sensitivity Tests; D018716:Molecular Mimicry; D015394:Molecular Structure; D015242:Ofloxacin / Q000494:pharmacology*; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D010446:Peptide Fragments; D064704:Levofloxacin; D015242:Ofloxacin