• Publications
  • Influence
Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide
There presently is no rapid method to assess the bactericidal activity of new regimens for tuberculosis. This study examined PNU-100480, TMC207, PA-824, SQ109, and pyrazinamide, singly and in variousExpand
  • 63
  • 5
Mycobactericidal Activity of Sutezolid (PNU-100480) in Sputum (EBA) and Blood (WBA) of Patients with Pulmonary Tuberculosis
Rationale Sutezolid (PNU-100480) is a linezolid analog with superior bactericidal activity against Mycobacterium tuberculosis in the hollow fiber, whole blood and mouse models. Like linezolid, it isExpand
  • 82
  • 3
  • PDF
Biomarker-Assisted Dose Selection for Safety and Efficacy in Early Development of PNU-100480 for Tuberculosis
ABSTRACT Tuberculosis is a serious global health threat for which new treatments are urgently needed. This study examined the safety, tolerability, pharmacokinetics, and pharmacodynamics of multipleExpand
  • 94
  • 2
  • PDF
Sensitization of bacteria to danofloxacin by temperate prophages.
Danofloxacin (CP-76,136) is in a class of agents that inhibit DNA gyrase and trigger induction of the SOS response and temperate bacteriophages. Killing studies against the bovine pathogenExpand
  • 15
  • 2
  • PDF
Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers.
BACKGROUND The oxazolidinone PNU-100480 is superior to linezolid against experimental murine tuberculosis. Two metabolites contribute to but do not fully account for its superiority. This studyExpand
  • 79
  • 1
Studies on time-kill kinetics of different classes of antibiotics against veterinary pathogenic bacteria including Pasteurella, Actinobacillus and Escherichia coli.
A systematic analysis of the bacteriostatic/bactericidal effect of several antibiotics used in veterinary medicine was carried out by time-kill kinetic analysis using P. haemolytica, P. multocida, A.Expand
  • 30
  • 1
5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COXExpand
  • 43
Structure-activity relationships of hygromycin A and its analogs: protein synthesis inhibition activity in a cell free system.
Several analogs of hygromycin A were tested in an Escherichia coli cell free protein synthesis inhibition assay and in a Serpulina hyodysenteriae whole cell assay. The aminocyclitol moiety isExpand
  • 32
  • PDF
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to theExpand
  • 32