Omega-conotoxin GVIA mimetics based on an anthranilamide core: effect of variation in ammonium side chain lengths and incorporation of fluorine.

@article{Andersson2009OmegaconotoxinGM,
  title={Omega-conotoxin GVIA mimetics based on an anthranilamide core: effect of variation in ammonium side chain lengths and incorporation of fluorine.},
  author={{\AA}sa Andersson and Jonathan B. Baell and Peter J Duggan and Janease E. Graham and Richard J Lewis and Natalie G. Lumsden and Charlotte Elisabet Tranberg and Kellie L. Tuck and Aijun Yang},
  journal={Bioorganic & medicinal chemistry},
  year={2009},
  volume={17 18},
  pages={6659-70}
}
A number of omega-conotoxin GVIA mimetics based on an anthranilamide core were prepared and tested for their affinity for rat brain Ca(v)2.2 channels. Features such as the presence of hydroxyl and fluoro substituents on the tyrosine side chain mimic, the length of the chains on the lysine/arginine side chain mimics and the use of diguanidino and diamino substituents rather than mono-guanidine/mono-amine substitution were examined. The diguanidinylated compounds proved to be the most active and… CONTINUE READING