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Synthesis and stability of S‐(2‐carboxyethyl)‐N‐(2‐t‐butyl‐5‐methoxy‐benzthiazol‐6‐yl)‐[ 14 C]dithiocarbamate [CGP 20376 (CGI 16483)]
Author(s) -
Anjaneyulu B.
Publication year - 1987
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580240811
Subject(s) - chemistry , dithiocarbamate , isothiocyanate , thiocyanate , potassium thiocyanate , medicinal chemistry , stereochemistry , ring (chemistry) , biological activity , chemical synthesis , in vitro , organic chemistry , biochemistry
For pharmacokinetic and metabolism studies in laboratory animals, CGP 20376 labelled with carbon‐14 on the dithiocarbamoyl carbon atom in the side chain at 6‐position of the benzthiazolyl ring system and having a specific activity of 6.13 μCi/mg (2.35 mCi/mmol) was synthesized, in four steps, starting with potassium[ 14 C]thiocyanate. At physiological pH ( in vitro ) [ 14 C] CGP 20376 dissociated rapidly into its biologically active isothiocyanate precursor [ 14 C] CGP 20308, indicating that it might behave as a pro‐drug.