Labeling strategies of selected subtypes of the hexahydronaphth[2,3‐b]‐1,4‐oxazine‐ and octahydrobenzo[<i>g</i>]quinoline‐type

Moenius, Thomas; Andres, Hendrik; Nozulak, Joachim; Salter, Rhys; Ray, Tridip; Burtscher, P.; Schnelli, Peter; Züger, Christoph; Voges, Rolf

doi:10.1002/jlcr.1310

Cited by 1 publication

(1 citation statement)

References 6 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The application of rapid labelling techniques allows the possibility of evaluating a whole series of compounds, either by tritiation of the whole series or of key members. Thus, Ho prepared a series of seven PEGylated‐peptides via a reactive 3 H‐labelled β‐alanine‐containing maleimide hapten (12), whereas Moenius and co‐workers synthesised a series of tricyclic central nervous system agents via reduction of a β‐ketoester function with tritiated Schwartz's reagent or by catalytic reduction of unsaturated precursors …”

Section: Discussionmentioning

confidence: 99%

Tritium: a coming of age for drug discovery and development ADME studies

Lockley

McEwen

Cooke

2012

Labelled Comp Radiopharmac

121

View full text Add to dashboard Cite

Owing to recent developments in tritium chemistry and analysis, high‐quality tritium‐labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery in adsorption, distribution, metabolism and excretion (ADME) projects. Such 3H‐labelled drugs are enabling high‐quality decision‐making at key points in the drug discovery process, thus ensuring more effective research projects, a key issue in commercial success. In addition, tritium‐labelled compounds continue to play a significant role in ADME studies later in the pharmaceutical development process. This is especially so for highly potent and hence low‐dose agents, for drugs with complex structures and for those compounds that undergo molecular fragmentation as a result of metabolism.

show abstract

Section: Discussionmentioning

confidence: 99%