Synthesis and structure of symmetrical bicyclic hexapeptides bridged by metathesis reaction

Org Lett. 2004 Sep 30;6(20):3449-52. doi: 10.1021/ol0487940.

Abstract

[structure: see text] Bicyclic hexapeptides 1a-c were synthesized via an intramolecular ring-closing metathesis reaction on solid phase followed by an N- to C-terminal cyclization in solution. Structural elucidation showed that these compounds assumed a C2-symmetrical structure with two beta-turns. The trans-ethylene plane was found to occupy two positions in rapid interconversion. One of the bicyclic hexapeptides crystallized with five water molecules, which made an arch above the ethylene group.

MeSH terms

  • Cyclization
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / chemistry
  • Protein Conformation*
  • Stereoisomerism

Substances

  • Peptides, Cyclic