Issue 6, 2019

Synthesis and biological evaluation of fluorinated analogues of ripostatin A

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

Supplementary files

Article information

Article type
Communication
Submitted
19 nov. 2018
Accepted
10 déc. 2018
First published
10 déc. 2018

Org. Biomol. Chem., 2019,17, 1362-1364

Synthesis and biological evaluation of fluorinated analogues of ripostatin A

V. Shenderman and E. V. Prusov, Org. Biomol. Chem., 2019, 17, 1362 DOI: 10.1039/C8OB02890G

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