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Synthesis of covalent [ 14 C]‐labeled diarylsulfonylurea (DASU) inhibitors of the processing and release of IL‐1
Author(s) -
Eggler J. F.,
Gabel C. A.,
Zandi K.,
Weaver J. D.,
McKechney H.,
Dombroski M. A.,
Peurano H.,
Hawryluk N.
Publication year - 2002
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.602
Subject(s) - chemistry , phosgene , covalent bond , sulfonamide , epoxide , combinatorial chemistry , chemical synthesis , stereochemistry , biochemistry , organic chemistry , in vitro , catalysis
CP‐452,759 and CP‐470,947, two covalent [ 14 C]‐labeled diarylsulfonylurea (DASU) inhibitors of the processing and release of IL‐1 from human monocytes, have been synthesized. The radiosyntheses utilize [ 14 C]‐labeled phosgene to prepare labeled isocyanates which are coupled with an epoxide sulfonamide to give the [ 14 C]‐DASUs. These tools should allow future studies aimed at purifying and identifying the DASU binding protein involved in the inhibition of the processing and release of IL‐1 from human monocytes. Copyright © 2002 John Wiley & Sons, Ltd.