Potent and selective CC chemokine receptor 1 antagonists labeled with carbon‐13, carbon‐14, and tritium | Zendy

Latli Bachir | Zendy; Hrapchak Matt | Zendy; Cheveliakov Maxim | Zendy; Reeves Jonathan T. | Zendy; Marsini Maurice | Zendy; Busacca Carl A. | Zendy; Senanayake Chris H. | Zendy

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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.

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