Low molecular weight non-peptide mimics of omega-conotoxin GVIA

Bioorg Med Chem Lett. 2009 May 15;19(10):2763-5. doi: 10.1016/j.bmcl.2009.03.130. Epub 2009 Mar 28.

Abstract

We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide omega-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193g/mol compared to a previously reported lead. This compound exhibits an EC(50) of 5.8microM and is accessible in only six synthetic steps compared to the original lead (13 steps). We also report several improvements to the original synthetic route.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / chemistry
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, N-Type / chemistry
  • Calcium Channels, N-Type / metabolism
  • Molecular Weight
  • Rats
  • omega-Conotoxin GVIA / chemistry*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, N-Type
  • omega-Conotoxin GVIA