Synthesis of a tritium‐labeled photo‐affinity probe based on an atypical leukotriene biosynthesis inhibitor | Zendy

Kumar Nag S. | Zendy; Braun Matthew P. | Zendy; Chaudhary Ashok G. | Zendy; Young Robert N. | Zendy

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Synthesis of a tritium‐labeled photo‐affinity probe based on an atypical leukotriene biosynthesis inhibitor

Author(s) -

Kumar Nag S.,

Braun Matthew P.,

Chaudhary Ashok G.,

Young Robert N.

Publication year - 2011

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.1804

Subject(s) - chemistry , tritium , biosynthesis , thiazole , triethylamine , anhydrous , radiosynthesis , stereochemistry , combinatorial chemistry , biochemistry , organic chemistry , enzyme , physics , microbiology and biotechnology , in vivo , nuclear physics , biology

A radiolabeled photo‐affinity probe containing a diazirine group was designed and synthesized based on an atypical leukotriene (LT) biosynthesis inhibitor to determine whether this type of inhibitor (such as 5) interacts with a novel protein, critical for LT biosynthesis. One of the key transformations was to introduce a tritium label in the thiazole ring. This was eventually achieved by treating the iodinated compound with tritium, Pt/C (sulfided) and triethylamine in anhydrous aprotic solvent, to give the tritiated compound with a specific activity of 303 GBq/mmol. The affinity probe will be used to identify the proteins and protein complexes with which this type of molecules interacts with in inflammatory cells. Copyright © 2010 John Wiley & Sons, Ltd.

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