A simple in vitro assay for assessing the reactivity of nitrile containing compounds.
A quantitative assay involving the reaction of nitriles with glutathione and cysteine has been used as a simple in vitro screen to assess potential toxicity risk of candidate compounds in drug discovery. Studies have indicated that, when benchmarked with selected compounds, the reaction of the nitriles with glutathione can provide a useful tool for deciding whether or not to progress compounds in the absence of radiolabelling studies.
MacFaul
Philip A
PA
AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. Philip.MacFaul@astrazeneca.com
Morley
Andrew D
AD
Crawford
James J
JJ
D003545:Cysteine / Q000032:analysis / Q000633:toxicity; D055808:Drug Discovery; D005978:Glutathione / Q000032:analysis / Q000633:toxicity; D015394:Molecular Structure; D009543:Nifedipine / Q000031:analogs & derivatives / Q000494:pharmacology; D009570:Nitriles / Q000032:analysis / Q000633:toxicity*
D009570:Nitriles; C035100:nilvadipine; D005978:Glutathione; D009543:Nifedipine; D003545:Cysteine