Skip to search formSkip to main contentSkip to account menu
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.
TLDR
Sulfonamide 56 (UK-421,045) was selected as a candidate for further preclinical evaluation as a topically applied, dermal anti-scarring agent and demonstrates excellent selectivity over MMPs involved in wound healing (>10 000-fold).
View on PubMed
Pre-clinical pharmacokinetics of UK-453,061, a novel non-nucleoside reverse transcriptase inhibitor (NNRTI), and use of in silico physiologically based prediction tools to predict the oral…
TLDR
This study demonstrates the utility of using in silico PBPK approaches to make predictions of human pharmacokinetics before dosing for the first time in humans.
View on PubMed
Comparison of the Non‐Nucleoside Reverse Transcriptase Inhibitor Lersivirine with its Pyrazole and Imidazole Isomers
TLDR
The pharmacological and pharmacokinetic profile of lersivirine with its pyrazole and imidazole isomers is compared and established as the outstanding molecule in this set.
View on Wiley
Pre-clinical pharmacokinetics of UK-453,061, a novel non-nucleoside reverse transcriptase inhibitor (NNRTI), and use of in silico physiologically based prediction tools to predict the oral…
TLDR
This study demonstrates the utility of using in silico PBPK approaches to make predictions of human pharmacokinetics before dosing for the first time in humans.
View on Taylor & Francis
Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: A rationale for long-lived plasma radioactivity
TLDR
Data indicate that this metabolite results from the oxadiazole ring-cleavage-producing oxamic acid, oxamide and oxalic acid, and was identified as the long-lived radioactivity which was observed in dog plasma.
View on Taylor & Francis
Case studies addressing human pharmacokinetic uncertainty using a combination of pharmacokinetic simulation and alternative first in human paradigms
TLDR
A retrospective analysis of the data showed that, if the tools had been available at the time, the pharmacokinetics of PF-184298 in human could have been predicted from a population based simulation tool in combination with physicochemical properties and in vitro human intrinsic clearance.
View on Taylor & Francis
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
TLDR
A novel series of indazole NNRTIs that possess excellent metabolic stability and mutant resilience and structure-based drug design techniques are created.
View on PubMed
Optimization of 5‐Aryloxyimidazole Non‐Nucleoside Reverse Transcriptase Inhibitors
TLDR
This work presents the optimization of a series of 5‐aryloxy imidazoles, which possess a balanced pharmacological profile against both wild‐type enzyme and the clinically relevant mutations K103N and Y181C.
View on Wiley
Pharmacokinetic/pharmacodynamic assessment of the effects of E4031, cisapride, terfenadine and terodiline on monophasic action potential duration in dog
TLDR
Data indicate that the free ED50 in plasma for terfenadine, terodiline, cisapride and E4031 closely correlate with the free concentration in man causing QT effects, underline the need to maximize the therapeutic ratio with respect to TDP in potential development candidates and the importance of using free drug concentrations in pharmacokinetic/pharmacodynamic studies.
View on Taylor & Francis
Determination of flutamide and hydroxyflutamide in dog plasma by a sensitive high performance liquid chromatography method utilizing mid-bore chromatography.
TLDR
The method described demonstrates a cost-effective means of determining both components while maintaining excellent sensitivity and resolution and the utilization of mid-bore chromatography increases the method sensitivity while simultaneously conserving on the quantities of mobile phase required for analysis and subsequent disposal of as hazardous waste.
View on PubMed
...
...
By clicking accept or continuing to use the site, you agree to the terms outlined in our Privacy Policy, Terms of Service, and Dataset License