• Publications
  • Influence
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.
Drug therapy is the mainstay of antimalarial therapy, yet current drugs are threatened by the development of resistance. In an effort to identify new potential antimalarials, we have undertaken aExpand
  • 207
  • 5
3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.
A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library.Expand
  • 100
  • 2
Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability for the development of novel oxazolidinones
1. Allometric scaling has previously been used as an effective tool for the prediction of human pharmacokinetic data. The pharmacokinetic data for linezolid, a novel oxazolidinone to treatExpand
  • 14
A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders
Nicotinamide N-methyltransferase (NNMT) is a cytosolic enzyme that catalyzes the transfer of a methyl group from the co-factor S-adenosyl-L-methionine (SAM) onto the substrate, nicotinamide (NA) toExpand
  • 17
Pre-clinical assessment of DRF 4367, a novel COX-2 inhibitor: Evaluation of pharmacokinetics, absolute oral bioavailability and metabolism in mice and comparative inter-species in vitro metabolism
The aim of this study was to characterize the pharmacokinetics and determine the absolute bioavailability and metabolism of DRF 4367, a novel COX-2 inhibitor, in mice. In addition, the in vitroExpand
  • 8
  • PDF
Sensitive LC-MS/MS Method for the Simultaneous Determination of Bendamustine and its Active Metabolite, γ-Hydroxybendamustine in Small Volume Mice and Dog Plasma and its Application to a
A highly sensitive, specific and rapid LC-ESI-MS/MS method has been developed and validated for the simultaneous quantification of bendamustine (BM) and γ-hydroxybendamustine (HBM) in small volumeExpand
  • 8
Simultaneous determination of OZ277, a synthetic 1,2,4-trioxolane antimalarial, and its polar metabolites in rat plasma using hydrophilic interaction chromatography.
OZ277 is a synthetic 1,2,4-trioxolane antimalarial currently being evaluated in clinical trails. Biotransformation of OZ277 in rats results in the generation of metabolites with large differences inExpand
  • 9
Interspecies scaling of urinary excretory amounts of nine drugs belonging to different therapeutic areas with diverse chemical structures – accurate prediction of the human urinary excretory amounts
Abstract 1. The human urinary excretory amounts of total drug (parent + metabolites) were predicted for nine drugs with diverse chemical structures using simple allometry. The drugs used for scalingExpand
  • 7
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation.
Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the 2-position led to identification ofExpand
  • 6