Chemoenzymatic Synthesis of Trehalosamine, an Aminoglycoside Antibiotic and Precursor to Mycobacterial Imaging Probes

J Org Chem. 2018 Aug 3;83(15):8662-8667. doi: 10.1021/acs.joc.8b00810. Epub 2018 Jul 23.

Abstract

Trehalosamine (2-amino-2-deoxy-α,α-d-trehalose) is an aminoglycoside with antimicrobial activity against Mycobacterium tuberculosis, and it is also a versatile synthetic intermediate used to access imaging probes for mycobacteria. To overcome inefficient chemical synthesis approaches, we report a two-step chemoenzymatic synthesis of trehalosamine that features trehalose synthase (TreT)-catalyzed glycosylation as the key transformation. Soluble and recyclable immobilized forms of TreT were successfully employed. We demonstrate that chemoenzymatically synthesized trehalosamine can be elaborated to two complementary imaging probes, which label mycobacteria via distinct pathways.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Sugars / chemical synthesis*
  • Amino Sugars / chemistry
  • Amino Sugars / metabolism*
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism*
  • Biocatalysis
  • Chemistry Techniques, Synthetic
  • Glucosyltransferases / metabolism*
  • Glycosylation
  • Molecular Imaging*
  • Mycobacterium tuberculosis / metabolism*

Substances

  • Amino Sugars
  • Anti-Bacterial Agents
  • trehalosamine
  • Glucosyltransferases
  • trehalose synthase