Total Synthesis and Biological Evaluation of the Anti-Inflammatory (13 R,14 S,15 R)-13-Hydroxy-14-deoxyoxacyclododecindione

J Nat Prod. 2023 Apr 28;86(4):924-938. doi: 10.1021/acs.jnatprod.2c01145. Epub 2023 Mar 31.

Abstract

The first total synthesis of the natural product (13R,14S,15R)-13-hydroxy-14-deoxyoxacyclododecindione, which was isolated in 2018 as a member of the oxacyclododecindione family, is reported. A synthetic strategy through intramolecular Friedel-Crafts acylation combined with the stereoselective synthesis of a new triol key fragment allowed the preparation of the macrolactone. Due to mismatching physical data of the synthetic product, a revision of the configuration of the natural product isolated in 2018 is required. Light-induced E/Z-isomerism of the macrolactone backbone is described for the first time in the class of oxacyclododecindione-type macrolactones. The hydroxylated macrolactone prepared herein was found to show highly promising IC50 values in biological assays addressing the inhibition of inflammatory responses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents* / pharmacology
  • Isomerism
  • Molecular Structure
  • Stereoisomerism

Substances

  • Anti-Inflammatory Agents
  • (13R,14S,15R)-13-hydroxy-14-deoxyoxacyclododecindione