Research Topics
| Thomas E RenauSummaryAffiliation: F. Hoffmann-La Roche Ltd Publications
| Collaborators
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Detail Information
Publications
Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosaThomas E Renau
Essential Therapeutics, Inc, 850Maude Avenue, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 12:763-6. 2002..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...
MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: discovery and early strategies for lead optimizationKiyoshi Nakayama
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co, Ltd, 1 16 13, Kitakasai, Edogawa, Tokyo, 134 8630, Japan
Bioorg Med Chem Lett 13:4201-4. 2003..Early leads lacked activity in animal models, and efforts to improve solubility and reduce serum protein binding by the introduction of polar groups are discussed...
Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosaThomas E Renau
Essential Therapeutics, Inc, 850Maude Avenue, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 13:2755-8. 2003....
The potential of phosphodiesterase 4 inhibitors for the treatment of depression: opportunities and challengesThomas E Renau
Roche Palo Alto, 3431 Hillview Ave, Palo Alto, CA 94304, USA
Curr Opin Investig Drugs 5:34-9. 2004..The following review examines the promise that PDE4 inhibitors may hold for the treatment of these diseases...
The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitorsWilliam J Watkins
Essential Therapeutics, Inc, 850Maude Ave, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 13:4241-4. 2003..The ratio of drug levels in tissue versus serum was not significantly reduced in any of the active analogues examined...
Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivativesWilliam J Watkins
Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 14:5133-7. 2004....
Molecular basis for fungal selectivity of novel antimitotic compoundsThomas Lila
Essential Therapeutics, Mountain View, California 94043, USA
Antimicrob Agents Chemother 47:2273-82. 2003..Features of the proposed binding site explain the observed fungal tubulin specificity of the series and are consistent with structure-activity relationships among a library of related compounds...
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffoldsKiyoshi Nakayama
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co, Ltd, 1 16 13, Kitakasai, Edogawa, Tokyo 134 8630, Japan
Bioorg Med Chem Lett 13:4205-8. 2003....
