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Potent and selective CC chemokine receptor 1 antagonists labeled with carbon‐13, carbon‐14, and tritium
Author(s) -
Latli Bachir,
Hrapchak Matt,
Cheveliakov Maxim,
Reeves Jonathan T.,
Marsini Maurice,
Busacca Carl A.,
Senanayake Chris H.
Publication year - 2018
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.3635
Subject(s) - tritium , chemistry , ccr1 , pyridine , amide , cc chemokine receptors , carbon 14 , chemokine , combinatorial chemistry , stereochemistry , receptor , medicinal chemistry , chemokine receptor , organic chemistry , biochemistry , physics , quantum mechanics , nuclear physics
1‐(4‐Fluorophenyl)‐1 H ‐pyrazolo[3,4‐c]pyridine‐4‐carboxylic acid (2‐methanesulfonyl‐pyridin‐4‐ylmethyl)‐amide ( 1 ) and its analogs ( 2 ) and ( 3 ) are potent CCR1 antagonists intended for the treatment of rheumatoid arthritis. The detailed syntheses of these 3 compounds labeled with carbon‐13 as well as the preparation of ( 1 ) and ( 2 ) labeled with carbon‐14, and ( 1 ) labeled with tritium, are described.