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Synthesis and biological evaluation of fluorinated analogues of ripostatin A

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Abstract

Several monocyclic derivatives of 14,14′-difluororipostatin A were prepared using a catalytic Mukaiyama aldol reaction, a ring-closing metathesis reaction and a late stage click reaction as key steps. The biological activity of the produced compounds was assessed in vivo using a panel of pathogenic microorganisms. Moderate antibiotic activity was observed for 11-OMe-ripostatin A and 11-OMe-14,14′-difluororipostatin A.

Graphical abstract: Synthesis and biological evaluation of fluorinated analogues of ripostatin A

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Publication details

The article was received on 19 Nov 2018, accepted on 10 Dec 2018 and first published on 10 Dec 2018


Article type: Communication
DOI: 10.1039/C8OB02890G
Citation: Org. Biomol. Chem., 2019, Advance Article
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    Synthesis and biological evaluation of fluorinated analogues of ripostatin A

    V. Shenderman and E. V. Prusov, Org. Biomol. Chem., 2019, Advance Article , DOI: 10.1039/C8OB02890G

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