Design, synthesis, and biological evaluation of biotin-labeled (−)-ternatin, a potent fat-accumulation inhibitor against 3T3-L1 adipocytes

The design, synthesis, and biological activity of biotin-labeled (−)-ternatin are reported. Chemical modification, that is, biotinylation, was conducted using Click chemistry at the 6-position (NMe-d-ProGly moiety), which was a plausible location selected on the basis of our SAR studies. The compound displayed sufficient fat-accumulation inhibitory effect against 3T3-L1 adipocytes for further bio-organic studies.

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